Imatinib

別名：STI571, CGP-57148B

製品コード：S2475 純度：99.97%

Imatinib is a multi-target inhibitor of tyrosine kinase with inhibition for v-Abl, c-Kit and PDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) induces autophagy.

CAS No. 152459-95-5

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
250mg	JPY 22000	国内在庫あり
1g	JPY 44500	国内在庫あり

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（304）

製品安全説明書

現在のバッチを見る：純度： 99.97%

99.97

Imatinib関連製品

関連ターゲット	PDGFRα PDGFRβ	もっと見る
関連製品	Crenolanib CP-673451 Orantinib (SU6668) Tyrphostin AG 1296 Trapidil PP121 AZD2932	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library PI3K/Akt Inhibitor Library Cell Cycle compound library Angiogenesis Related compound Library	もっと見る

シグナル伝達経路

PDGFRシグナル伝達経路

PDGFR阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
BA/F3	Antiproliferative assay	5 to 10 uM	48 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Tel-SH2-KD assessed as cell viability at 5 to 10 uM after 48 hrs by MTT assay, IC50=0.055μM.	16415863
BA/F3	Antiproliferative assay	5 to 10 uM	48 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Tel-SH3-SH2-KD assessed as cell viability at 5 to 10 uM after 48 hrs by MTT assay, IC50=0.088μM.	16415863
BA/F3	Antiproliferative assay	5 to 10 uM	48 hrs	Antiproliferative activity against mouse BA/F3 cells expressing NPM-abl assessed as cell viability at 5 to 10 uM after 48 hrs by MTT assay, IC50=0.393μM.	16415863
Ba/F3	Function assay	1 uM	24 hrs	Inhibition of 14-3-3sigma in human Ba/F3 cells expressing wild type Bcr-Abl construct assessed as release of full-length c-Abl from cytoplasmic complex with 14-3-3sigma at 1 uM after 24 hrs by immunoprecipitation/immunoblot technique	21962576
Ba/F3	Function assay	1 uM	24 hrs	Inhibition of 14-3-3sigma in human Ba/F3 cells expressing wild type Bcr-Abl construct assessed as nuclear import of full-length c-Abl at 1 uM after 24 hrs by immunoprecipitation/immunoblot technique	21962576
K562	Function assay	40 uM	6 hrs	Inhibition of BCR-ABL-mediated ERK1 phosphorylation in human K562 cells at 40 uM after 6 hrs by phospho-flow cytometry	22148584
K562	Function assay	40 uM	6 hrs	Inhibition of BCR-ABL-mediated ERK2 phosphorylation in human K562 cells at 40 uM after 6 hrs by phospho-flow cytometry	22148584
HEK293	Function assay	500 uM	1.5 mins	Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells up to 500 uM after 1.5 mins by fluorescence assay, IC50=0.35μM.	23241029
BA/F3	Antitumor assay	50 mg/kg	14 days	Antitumor activity against mouse BA/F3 cells expressing wild type BCR-ABL allografted in SCID mouse assessed as inhibition of tumor growth at 50 mg/kg, po qd for 14 days	23301703
K562	Function assay	10 uM	1 hr	Inhibition of Bcr/Abl kinase tyrosine phosphorylation in human K562 cells at 10 uM after 1 hr by immunoblot analysis	24681986
K562	Function assay	10 uM	1 hr	Inhibition of Abl kinase tyrosine phosphorylation in human K562 cells at 10 uM after 1 hr by immunoblot analysis	24681986
K562	Function assay	10 uM	1 hr	Inhibition of tyrosine phosphorylation of protein with molecular weight between 40 and 60 kDa in human K562 cells at 10 uM after 1 hr by immunoblot analysis	24681986
K562	Function assay	100 uM	8 hrs	Inhibition of BCR-ABL signaling pathway in human K562 cells assessed as suppression of STAT5 phosphorylation at 100 uM after 8 hrs in presence of MeBS by Western blot analysis	27666635
K562	Function assay	100 uM	8 hrs	Inhibition of BCR-ABL in signaling pathway human K562 cells assessed as suppression of CrkL phosphorylation at 100 uM after 8 hrs in presence of MeBS by Western blot analysis	27666635
K562	Function assay	100 uM	8 hrs	Inhibition of BCR-ABL phosphorylation in human K562 cells at 100 uM after 8 hrs in presence of MeBS by Western blot analysis	27666635
K562	Cell cycle assay	1 uM	24 hrs	Cell cycle arrest in human K562 cells assessed as accumulation at G0/G1 phase at 1 uM after 24 hrs by propidium iodide/RNase staining based flow cytometry	27966954
KU812	Cell cycle assay	1 uM	12 hrs	Cell cycle arrest in human KU812 cells assessed as accumulation at G0/G1 phase at 1 uM after 12 hrs by propidium iodide/RNase staining based flow cytometry	27966954
MEG01	Cell cycle assay	1 uM	24 hrs	Cell cycle arrest in human MEG01 cells assessed as accumulation at G0/G1 phase at 1 uM after 24 hrs by propidium iodide/RNase staining based flow cytometry	27966954
GISTT1	Cell cycle assay	1 uM	24 hrs	Cell cycle arrest in human GISTT1 cells assessed as accumulation at G0/G1 phase at 1 uM after 24 hrs by propidium iodide/RNase staining based flow cytometry	27966954
GIST882	Cell cycle assay	1 uM	48 hrs	Cell cycle arrest in human GIST882 cells assessed as accumulation at G0/G1 phase at 1 uM after 48 hrs by propidium iodide/RNase staining based flow cytometry	27966954
GIST882	Function assay	1 uM	2 hrs	Inhibition of c-KIT mediated signaling pathways assessed as reduction in AKT phosphorylation at S473 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting	27966954
GISTT1	Function assay	1 uM	2 hrs	Inhibition of c-KIT autophosphorylation at Y703 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting	27966954
GISTT1	Function assay	1 uM	2 hrs	Inhibition of c-KIT autophosphorylation at Y719 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting	27966954
GISTT1	Function assay	1 uM	2 hrs	Inhibition of c-KIT autophosphorylation at Y823 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting	27966954
GIST882	Function assay	1 uM	2 hrs	Inhibition of c-KIT autophosphorylation at Y703 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting	27966954
GIST882	Function assay	1 uM	2 hrs	Inhibition of c-KIT autophosphorylation at Y719 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting	27966954
GIST882	Function assay	1 uM	2 hrs	Inhibition of c-KIT autophosphorylation at Y823 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting	27966954
GISTT1	Function assay	1 uM	2 hrs	Inhibition of c-KIT mediated signaling pathways assessed as reduction in AKT phosphorylation at S473 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting	27966954
GISTT1	Function assay	1 uM	2 hrs	Inhibition of c-KIT mediated signaling pathways assessed as reduction in ERK1/2 phosphorylation at T202/Y204 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting	27966954
GISTT1	Function assay	1 uM	2 hrs	Inhibition of c-KIT mediated signaling pathways assessed as reduction in Stat3/5 phosphorylation at Y705/Y694 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting	27966954
GISTT1	Function assay	1 uM	2 hrs	Inhibition of c-KIT mediated signaling pathways assessed as reduction in S6 phosphorylation at S235/236 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting	27966954
GISTT1	Function assay	1 uM	2 hrs	Inhibition of c-KIT mediated signaling pathways assessed as reduction in S6K phosphorylation at T389 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting	27966954
GIST882	Function assay	1 uM	2 hrs	Inhibition of c-KIT mediated signaling pathways assessed as reduction in Stat3/5 phosphorylation at Y705/Y694 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting	27966954
GIST882	Function assay	1 uM	2 hrs	Inhibition of c-KIT mediated signaling pathways assessed as reduction in ERK1/2 phosphorylation at T202/Y204 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting	27966954
GIST882	Function assay	1 uM	2 hrs	Inhibition of c-KIT mediated signaling pathways assessed as reduction in S6 phosphorylation at S235/236 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting	27966954
GIST882	Function assay	1 uM	2 hrs	Inhibition of c-KIT mediated signaling pathways assessed as reduction in S6K phosphorylation at T389 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting	27966954
NCI-H1703	Function assay	1 uM	2 hrs	Inhibition of PDGF-induced PDGFRalpha autophosphorylation at Y1018 residue in human NCI-H1703 cells at 1 uM after 2 hrs in presence of PDGF-AA by Western blot analysis	29544149
NCI-H1703	Function assay	1 uM	2 hrs	Inhibition of PDGF-induced PDGFRalpha autophosphorylation at Y754 residue in human NCI-H1703 cells at 1 uM after 2 hrs in presence of PDGF-AA by Western blot analysis	29544149
NCI-H1703	Function assay	1 uM	2 hrs	Inhibition of PDGF-induced PDGFRalpha autophosphorylation at Y849 residue in human NCI-H1703 cells at 1 uM after 2 hrs in presence of PDGF-AA by Western blot analysis	29544149
EOL-1	Function assay	1 uM	2 hrs	Inhibition of PDGFRalpha in human EOL-1 cells assessed as decrease in STAT5 phosphorylation at Y694 residue at 1 uM after 2 hrs in presence of PDGF-AA by Western blot analysis	29544149
EOL-1	Function assay	1 uM	2 hrs	Inhibition of PDGFRalpha in human EOL-1 cells assessed as decrease in ERK phosphorylation at T202/Y204 residues at 1 uM after 2 hrs in presence of PDGF-AA by Western blot analysis	29544149
K562	Apoptosis assay	10 uM	48 hrs	Induction of apoptosis in human K562 cells assessed as increase in apoptotic cells at 10 uM incubated for 48 hrs by Caspase-3/7 reagent-based fluorescence assay	31097376
Neuro2a	Function assay	1 uM		Inhibition of DR24 in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis	26789657
K562	Apoptosis assay	1 uM		Induction of apoptosis in human K562 cells assessed as cleavage of PARP at 1 uM by Western blot analysis	27966954
K562	Apoptosis assay	1 uM		Induction of apoptosis in human K562 cells assessed as increase in cleaved caspase-3 level at 1 uM by Western blot analysis	27966954
KU812	Apoptosis assay	1 uM		Induction of apoptosis in human KU812 cells assessed as cleavage of PARP at 1 uM by Western blot analysis	27966954
KU812	Apoptosis assay	1 uM		Induction of apoptosis in human KU812 cells assessed as increase in cleaved caspase-3 level at 1 uM by Western blot analysis	27966954
MEG01	Apoptosis assay	1 uM		Induction of apoptosis in human MEG01 cells assessed as increase in cleaved caspase-3 level at 1 uM by Western blot analysis	27966954
GISTT1	Apoptosis assay	1 uM		Induction of apoptosis in human GISTT1 cells assessed as increase in cleaved caspase-3 level at 1 uM by Western blot analysis	27966954
MEG01	Apoptosis assay	1 uM		Induction of apoptosis in human MEG01 cells assessed as cleavage of PARP at 1 uM by Western blot analysis	27966954
GISTT1	Apoptosis assay	1 uM		Induction of apoptosis in human GISTT1 cells assessed as cleavage of PARP at 1 uM by Western blot analysis	27966954
GIST882	Apoptosis assay	1 uM		Induction of apoptosis in human GIST882 cells assessed as cleavage of PARP at 1 uM by Western blot analysis	27966954
GIST882	Apoptosis assay	1 uM		Induction of apoptosis in human GIST882 cells assessed as increase in cleaved caspase-3 level at 1 uM by Western blot analysis	27966954
K562	Function assay	1 uM		Inhibition of BCR-ABL in imatinib-sensitive human K562 cells assessed as decrease in CrKL phosphorylation at 1 uM by immuno blot analysis	30261468
BA/F3	Antiproliferative assay		48 hrs	Antiproliferative activity against mouse BA/F3 Bcr-abl negative cells expressing Tel-PDGFRbeta kinase assessed as proliferation after 48 hrs by MTT assay, IC50=0.027μM.	16415863
32D	Antiproliferative assay		48 hrs	Antiproliferative activity against mouse 32D cells transfected with p210 cells expressing Bcr-abl assessed as proliferation after 48 hrs by MTT assay, IC50=0.112μM.	16415863
BA/F3	Antiproliferative assay		48 hrs	Antiproliferation activity against mouse BA/F3 cells expressing Bcr-abl assessed as cell viability after 48 hrs by MTT assay, IC50=0.19μM.	16415863
BA/F3	Antiproliferative assay		48 hrs	Antiproliferative activity against mouse BA/F3 cells transfected with p210 Bcr-abl assessed as proliferation after 48 hrs by MTT assay, IC50=0.19μM.	16415863
M07e	Antiproliferative assay		48 hrs	Antiproliferative activity against human M07e Bcr-abl negative cells expressing stem cell factor assessed as proliferation after 48 hrs by MTT assay, IC50=0.257μM.	16415863
BA/F3	Antiproliferative assay		48 hrs	Antiproliferation activity against mouse BA/F3 cells expressing Bcr-abl A337N mutant assessed as cell viability after 48 hrs by MTT assay, IC50=0.339μM.	16415863
BA/F3	Antiproliferative assay		48 hrs	Antiproliferation activity against mouse BA/F3 cells expressing Bcr-abl A334l mutant assessed as cell viability after 48 hrs by MTT assay, IC50=0.962μM.	16415863
Vero	Antiviral assay		3 days	Antiviral activity against Dengue virus infected in african green monkey Vero cells administered before viral challenge after 3 days by viral plaque assay	17360676
EOL-1	Cytotoxicity assay		72 hrs	Cytotoxicity against human EOL-1 cells after 72 hrs by alamar-blue cell viability assay, IC50=0.0001995μM.	19301902
EOL-1	Cytotoxicity assay		72 hrs	Cytotoxicity against human EOL-1 cells after 72 hrs by alamar-blue cell viability assay, IC50=0.0002μM.	19301902
K562	Cytotoxicity assay		72 hrs	Cytotoxicity against human K562 cells after 72 hrs by alamar-blue cell viability assay, IC50=0.049μM.	19301902
K562	Cytotoxicity assay		72 hrs	Cytotoxicity against human K562 cells after 72 hrs by alamar-blue cell viability assay, IC50=0.1μM.	19301902
HCT116	Cytotoxicity assay		72 hrs	Cytotoxicity against human HCT116 cells after 72 hrs by alamar-blue cell viability assay, IC50=10μM.	19301902
RKOp21	Cytotoxicity assay		72 hrs	Cytotoxicity against human RKOp21 cells after 72 hrs by alamar-blue cell viability assay, IC50=12μM.	19301902
RKOp21	Cytotoxicity assay		72 hrs	Cytotoxicity against human RKOp21 cells after 72 hrs by alamar-blue cell viability assay, IC50=12.5892μM.	19301902
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by alamar-blue cell viability assay, IC50=15.5μM.	19301902
MDA-MB-468	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-468 cells after 72 hrs by alamar-blue cell viability assay, IC50=15.8489μM.	19301902
MDA-MB-468	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-468 cells after 72 hrs by alamar-blue cell viability assay, IC50=17μM.	19301902
HeLa	Cytotoxicity assay		72 hrs	Cytotoxicity against human HeLa cells after 72 hrs by alamar-blue cell viability assay, IC50=18.65μM.	19301902
Hec1A	Cytotoxicity assay		72 hrs	Cytotoxicity against human Hec1A cells after 72 hrs by alamar-blue cell viability assay, IC50=19μM.	19301902
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by alamar-blue cell viability assay, IC50=19.9526μM.	19301902
CAL27	Cytotoxicity assay		72 hrs	Cytotoxicity against human CAL27 cells after 72 hrs by alamar-blue cell viability assay, IC50=19.9526μM.	19301902
Hec1A	Cytotoxicity assay		72 hrs	Cytotoxicity against human Hec1A cells after 72 hrs by alamar-blue cell viability assay, IC50=19.9526μM.	19301902
CAL27	Cytotoxicity assay		72 hrs	Cytotoxicity against human CAL27 cells after 72 hrs by alamar-blue cell viability assay, IC50=22μM.	19301902
H460	Cytotoxicity assay		72 hrs	Cytotoxicity against human H460 cells after 72 hrs by alamar-blue cell viability assay, IC50=24μM.	19301902
PC3	Cytotoxicity assay		72 hrs	Cytotoxicity against human PC3 cells after 72 hrs by alamar-blue cell viability assay, IC50=24μM.	19301902
HCT15	Cytotoxicity assay		72 hrs	Cytotoxicity against human HCT15 cells after 72 hrs by alamar-blue cell viability assay, IC50=25μM.	19301902
HeLa	Cytotoxicity assay		72 hrs	Cytotoxicity against human HeLa cells after 72 hrs by alamar-blue cell viability assay, IC50=25.1189μM.	19301902
H460	Cytotoxicity assay		72 hrs	Cytotoxicity against human H460 cells after 72 hrs by alamar-blue cell viability assay, IC50=25.1189μM.	19301902
HCT15	Cytotoxicity assay		72 hrs	Cytotoxicity against human HCT15 cells after 72 hrs by alamar-blue cell viability assay, IC50=25.1189μM.	19301902
PC3	Cytotoxicity assay		72 hrs	Cytotoxicity against human PC3 cells after 72 hrs by alamar-blue cell viability assay, IC50=25.1189μM.	19301902
Saos2	Cytotoxicity assay		72 hrs	Cytotoxicity against human Saos2 cells after 72 hrs by alamar-blue cell viability assay, IC50=25.1189μM.	19301902
Saos2	Cytotoxicity assay		72 hrs	Cytotoxicity against human Saos2 cells after 72 hrs by alamar-blue cell viability assay, IC50=26μM.	19301902
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells after 72 hrs by alamar-blue cell viability assay, IC50=30μM.	19301902
A431	Cytotoxicity assay		72 hrs	Cytotoxicity against human A431 cells after 72 hrs by alamar-blue cell viability assay, IC50=31μM.	19301902
H69	Cytotoxicity assay		72 hrs	Cytotoxicity against human H69 cells after 72 hrs by alamar-blue cell viability assay, IC50=31.6228μM.	19301902
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells after 72 hrs by alamar-blue cell viability assay, IC50=31.6228μM.	19301902
A431	Cytotoxicity assay		72 hrs	Cytotoxicity against human A431 cells after 72 hrs by alamar-blue cell viability assay, IC50=31.6228μM.	19301902
H69	Cytotoxicity assay		72 hrs	Cytotoxicity against human H69 cells after 72 hrs by alamar-blue cell viability assay, IC50=32μM.	19301902
CCRF-CEM	Cytotoxicity assay		72 hrs	Cytotoxicity against human CCRF-CEM cells after 72 hrs by alamar-blue cell viability assay, IC50=36μM.	19301902
MDA-MB-231	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by alamar-blue cell viability assay, IC50=37μM.	19301902
CCRF-CEM/VCR1000	Cytotoxicity assay		72 hrs	Cytotoxicity against vincristine-resistant human CCRF-CEM/VCR1000 cells after 72 hrs by alamar-blue cell viability assay, IC50=37μM.	19301902
WM266.4	Cytotoxicity assay		72 hrs	Cytotoxicity against human WM266.4 cells after 72 hrs by alamar-blue cell viability assay, IC50=37μM.	19301902
U87MG	Cytotoxicity assay		72 hrs	Cytotoxicity against human U87MG cells after 72 hrs by alamar-blue cell viability assay, IC50=38μM.	19301902
SKBR3	Cytotoxicity assay		72 hrs	Cytotoxicity against human SKBR3 cells after 72 hrs by alamar-blue cell viability assay, IC50=39μM.	19301902
MDA-MB-231	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by alamar-blue cell viability assay, IC50=39.8107μM.	19301902
SKBR3	Cytotoxicity assay		72 hrs	Cytotoxicity against human SKBR3 cells after 72 hrs by alamar-blue cell viability assay, IC50=39.8107μM.	19301902
AsPC1	Cytotoxicity assay		72 hrs	Cytotoxicity against human AsPC1 cells after 72 hrs by alamar-blue cell viability assay, IC50=39.8107μM.	19301902
CCRF-CEM/VCR1000	Cytotoxicity assay		72 hrs	Cytotoxicity against vincristine-resistant human CCRF-CEM/VCR1000 cells after 72 hrs by alamar-blue cell viability assay, IC50=39.8107μM.	19301902
CCRF-CEM	Cytotoxicity assay		72 hrs	Cytotoxicity against human CCRF-CEM cells after 72 hrs by alamar-blue cell viability assay, IC50=39.8107μM.	19301902
U87MG	Cytotoxicity assay		72 hrs	Cytotoxicity against human U87MG cells after 72 hrs by alamar-blue cell viability assay, IC50=39.8107μM.	19301902
WM266.4	Cytotoxicity assay		72 hrs	Cytotoxicity against human WM266.4 cells after 72 hrs by alamar-blue cell viability assay, IC50=39.8107μM.	19301902
AsPC1	Cytotoxicity assay		72 hrs	Cytotoxicity against human AsPC1 cells after 72 hrs by alamar-blue cell viability assay, IC50=44μM.	19301902
A2780	Cytotoxicity assay		72 hrs	Cytotoxicity against human A2780 cells after 72 hrs by alamar-blue cell viability assay, IC50=48μM.	19301902
HT-29	Antiproliferative assay		96 hrs	Antiproliferative activity against human HT-29 cells after 96 hrs by SRB assay, IC50=0.06μM.	19469547
GIST882	Antiproliferative assay		96 hrs	Antiproliferative activity against human GIST882 cells after 96 hrs by SRB assay, IC50=1.7μM.	19469547
HGC27	Antiproliferative assay		96 hrs	Antiproliferative activity against human HGC27 cells after 96 hrs by SRB assay, IC50=2.4μM.	19469547
MCF7	Antiproliferative assay		96 hrs	Antiproliferative activity against human MCF7 cells after 96 hrs by SRB assay, IC50=11.5μM.	19469547
GIST48	Cytotoxicity assay		3 to 6 days	Cytotoxicity against human GIST48 cells assessed as effect on cell viability after 3 to 6 days by luciferase based luminescence assay, IC50=18.7μM.	19469547
KBM5	Cytotoxicity assay		72 hrs	Cytotoxicity against human KBM5 cells harboring wild type Bcr-Abl after 72 hrs by MTT assay, IC50=0.28μM.	20149665
KBM5	Cytotoxicity assay		72 hrs	Cytotoxicity against human KBM5 cells harboring Bcr-Abl T315I mutant after 72 hrs by MTT assay, IC50=5.4μM.	20149665
FDC-P1	Function assay		48 hrs	Inhibition of human FMS expressed in growth factor dependent mouse FDC-P1 cells assessed as inhibition of FMS-mediated cell proliferation in presence human CSF1 after 48 hrs by resazurin dye reduction assay, IC50=1.274μM.	20156689
FDC-P1	Function assay		48 hrs	Inhibition of mouse GM-CSF-stimulated cell proliferation of growth factor dependent mouse FDC-P1 cells expressing human FMS after 48 hrs by resazurin dye reduction assay, IC50=8.437μM.	20156689
K562	Function assay		2 hrs	Inhibition of BCR/ABL p210 autophosphorylation in human K562 cells after 2 hrs by Western blot analysis, IC50=0.75μM.	20188579
BESM	Antitrypanosomal assay		88 hrs	Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BESM cells measured after 88 hrs postinfection by HTS assay, EC50=9μM.	20547819
BESM	Cytotoxicity assay		88 hrs	Cytotoxicity against BESM cells after 88 hrs by HTS assay, EC50=32μM.	20547819
K562	Cytotoxicity assay		48 hrs	Cytotoxicity against human K562 cells after 48 hrs by MTT assay, IC50=0.58μM.	21295380
K562	Antiproliferative assay		48 hrs	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50=5.4μM.	21576023
K562	Function assay		6 hrs	Inhibition of BCR-ABL-mediated STAT5 phosphorylation in human K562 cells after 6 hrs by phospho-flow cytometry	22148584
primary leukemia cells	Cytotoxicity assay		72 hrs	Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing wild type FLT3 assessed as cell viability after 72 hrs by luciferase assay, IC50=0.1μM.	22221201
primary leukemia cells	Cytotoxicity assay		72 hrs	Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing FLT3-D835Y mutation assessed as cell viability after 72 hrs by luciferase assay, IC50=0.5μM.	22221201
K562	Cytotoxicity assay		24 hrs	Cytotoxicity against human K562 cells after 24 hrs by MTT assay, IC50=0.1μM.	22632935
K562	Cytotoxicity assay		48 to 72 hrs	Cytotoxicity against human BCR-ABL positive K562 cells after 48 to 72 hrs by MTT assay, IC50=0.3844μM.	22789429
K562	Cytotoxicity assay		72 hrs	Cytotoxicity against human K562 cells after 72 hrs by MTS assay, GI50=0.39μM.	22932313
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396P mutant after 72 hrs by CCK-8 assay, IC50=0.11μM.	23088644
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M244V mutant after 72 hrs by CCK-8 assay, IC50=0.129μM.	23088644
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E355G mutant after 72 hrs by CCK-8 assay, IC50=0.362μM.	23088644
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant after 72 hrs by CCK-8 assay, IC50=0.424μM.	23088644
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F359V mutant after 72 hrs by CCK-8 assay, IC50=0.96μM.	23088644
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253F mutant after 72 hrs by CCK-8 assay, IC50=1.444μM.	23088644
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay, IC50=1.834μM.	23088644
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl G250E mutant after 72 hrs by CCK-8 assay, IC50=1.863μM.	23088644
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396R mutant after 72 hrs by CCK-8 assay, IC50=2.377μM.	23088644
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F486S mutant after 72 hrs by CCK-8 assay, IC50=2.547μM.	23088644
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255K mutant after 72 hrs by CCK-8 assay, IC50=2.951μM.	23088644
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay, IC50=3.005μM.	23088644
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Q252H mutant after 72 hrs by CCK-8 assay, IC50=3.763μM.	23088644
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255V mutant after 72 hrs by CCK-8 assay, IC50=8.615μM.	23088644
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253H mutant after 72 hrs by CCK-8 assay, IC50=17.083μM.	23088644
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CCK-8 assay, IC50=18.52μM.	23088644
MDCK2	Function assay		5 mins	Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis, IC50=0.04μM.	23241029
HEK293	Function assay		1.5 mins	Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis, IC50=0.05μM.	23241029
HEK293	Function assay		1.5 mins	Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay, IC50=0.35μM.	23241029
HEK293	Function assay		1.5 mins	Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay, IC50=2.9μM.	23241029
HEK293	Function assay		3 mins	Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay, IC50=4.2μM.	23241029
HEK293	Function assay		3 mins	Inhibition of human OCT3-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay, IC50=25.5μM.	23241029
insect cells	Function assay		30 mins	Inhibition of human recombinant wild type ABL1 expressed in insect cells after 30 mins by FRET assay, IC50=0.0982μM.	23301703
insect cells	Function assay		30 mins	Inhibition of human recombinant ABL1 M351T mutant expressed in insect cells after 30 mins by FRET assay, IC50=0.1143μM.	23301703
insect cells	Function assay		30 mins	Inhibition of human recombinant ABL1 Q252H mutant expressed in insect cells after 30 mins by FRET assay, IC50=0.115μM.	23301703
insect cells	Function assay		30 mins	Inhibition of human recombinant ABL1 H396P mutant expressed in insect cells after 30 mins by FRET assay, IC50=0.1739μM.	23301703
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL M351T mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=0.24μM.	23301703
insect cells	Function assay		30 mins	Inhibition of human recombinant ABL1 G250E mutant expressed in insect cells after 30 mins by FRET assay, IC50=0.3599μM.	23301703
insect cells	Function assay		30 mins	Inhibition of human recombinant ABL1 E255K mutant expressed in insect cells after 30 mins by FRET assay, IC50=0.4858μM.	23301703
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing wild type BCR-ABL assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=0.5μM.	23301703
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E359V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=0.59μM.	23301703
insect cells	Function assay		30 mins	Inhibition of human recombinant ABL1 Y253F mutant expressed in insect cells after 30 mins by FRET assay, IC50=0.7496μM.	23301703
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F486S mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=1μM.	23301703
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E355G mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=1.6μM.	23301703
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317L mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=3.3μM.	23301703
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Q252H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=3.6μM.	23301703
insect cells	Function assay		30 mins	Inhibition of human recombinant ABL1 T315I mutant expressed in insect cells after 30 mins by FRET assay, IC50=5.155μM.	23301703
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL G250E mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=5.2μM.	23301703
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255K mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=5.6μM.	23301703
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253F mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=9.2μM.	23301703
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=9.5μM.	23301703
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL H396R mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=11.1μM.	23301703
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=12.2μM.	23301703
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL L248V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=12.2μM.	23301703
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=12.5μM.	23301703
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50=13.5μM.	23301703
BA/F3	Cytotoxicity assay		48 hrs	Cytotoxicity against mouse BA/F3 cells transfected with wild type Bcr-Abl after 48 hrs by XTT assay, IC50=0.092μM.	23600806
BA/F3	Cytotoxicity assay		48 hrs	Cytotoxicity against mouse BA/F3 cells transfected with Bcr-Abl T315I mutant after 48 hrs by XTT assay, IC50=4.79μM.	23600806
Ba/F3	Function assay		1 hr	Inhibition of Bcr-Abl T315I mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction of phosphorylated CrkL level after 1 hr by Western blot analysis	23600806
Ba/F3	Function assay		1 hr	Inhibition of Bcr-Abl T315I mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction of phosphorylated STAT5 level after 1 hr by Western blot analysis	23600806
Ba/F3	Function assay		1 hr	Inhibition of Bcr-Abl T315I mutant (unknown origin) phosphorylation transfected in mouse Ba/F3 cells after 1 hr by Western blot analysis	23600806
K562	Cytotoxicity assay		48 hrs	Cytotoxicity against human K562 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50=0.47μM.	23735826
GISTT1	Function assay		72 hrs	Inhibition of KIT in human GISTT1 cells assessed as growth inhibition after 72 hrs by SRB assay, GI50=0.01μM.	23773153
GIST48B	Growth inhibition assay		72 hrs	Growth inhibition of human GIST48B cells after 72 hrs by SRB assay, GI50=20μM.	23773153
K562	Antiproliferative assay		48 hrs	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50=0.5μM.	23932071
HepG2	Antiproliferative assay		24 to 96 hrs	Antiproliferative activity against human HepG2 cells after 24 to 96 hrs by MTS assay, IC50=10μM.	23932071
K562	Cytotoxicity assay		72 hrs	Cytotoxicity against human K562 cells after 72 hrs by calcein-AM assay, IC50=0.5μM.	23981532
K562	Antiproliferative assay		24 hrs	In vitro antiproliferative activity against human K562 cells assessed as decrease in cell viability after 24 hrs by MTT assay, IC50=13μM.	24681986
BV173	Antiproliferative assay		24 hrs	In vitro antiproliferative activity against human BV173 cells assessed as decrease in cell viability after 24 hrs by MTT assay, IC50=20μM.	24681986
CCRF-CEM	Antiproliferative assay		24 hrs	In vitro antiproliferative activity against human CCRF-CEM cells assessed as decrease in cell viability after 24 hrs by MTT assay, IC50=45μM.	24681986
HGC27	Cytotoxicity assay		48 hrs	Cytotoxicity against HGC27 cells assessed as cell viability after 48 hrs by MTT assay, IC50=3.8μM.	24900584
K562	Antiproliferative assay		48 hrs	Antiproliferative activity against Bcr/Abl positive human K562 cells after 48 hrs by MTT method, IC50=4.12μM.	25464886
K562	Cytotoxicity assay		72 hrs	Cytotoxicity against human K562 cells after 72 hrs using Calcein AM by fluorescence assay, IC50=0.5μM.	25757603
K562	Antiproliferative assay		48 hrs	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50=0.47μM.	25778766
K562	Antiproliferative assay		72 hrs	Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay, IC50=0.28μM.	26195136
K562	Antiproliferative assay		48 hrs	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50=1.16μM.	26231079
K562	Antiproliferative assay		48 hrs	Antiproliferative activity against imatinib-resistant human K562 cells after 48 hrs by MTT assay, IC50=15.7μM.	26231079
K562	Antiproliferative assay		48 hrs	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50=4.12μM.	26298495
K562	Cytotoxicity assay		48 hrs	Cytotoxicity against human K562 cells expressing Bcr-Abl assessed as growth inhibition after 48 hrs by MTT assay, IC50=1.16μM.	26451772
BA/F3	Growth inhibition assay		48 hrs	Growth inhibition of mouse BA/F3 cells expressing wild-type Bcr-Abl after 48 hrs by MTT assay, IC50=0.089μM.	26562217
BA/F3	Growth inhibition assay		48 hrs	Growth inhibition of mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 48 hrs by MTT assay, IC50=14.5μM.	26562217
K562	Antiproliferative assay		48 hrs	Antiproliferative activity against human K562 cells after 48 hrs by trypan blue dye exclusion assay, IC50=0.22μM.	26629859
K562	Apoptosis assay		48 hrs	Induction of apoptosis in human K562 cells after 48 hrs by annexinV and propidium iodide staining based flow cytometry, AC50=0.68μM.	26629859
K562	Cytotoxicity assay		48 hrs	Cytotoxicity against human K562 cells after 48 hrs by MTT assay, IC50=0.53μM.	26707846
K562	Cytotoxicity assay		72 hrs	Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by fluorescence microplate reader method, IC50=0.73μM.	26741853
K562	Antiproliferative assay		72 hrs	Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=0.14μM.	26789553
KU812	Antiproliferative assay		72 hrs	Antiproliferative activity against human KU812 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=0.16μM.	26789553
MEG01	Antiproliferative assay		72 hrs	Antiproliferative activity against human MEG01 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=0.24μM.	26789553
BA/F3	Function assay		72 hrs	Inhibition of BCR/ABL p210 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=0.38μM.	26789553
BA/F3	Function assay		72 hrs	Inhibition of TEL-LCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=0.5μM.	26789553
BA/F3	Function assay		72 hrs	Inhibition of BCR/ABL p210-M351T mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=0.625μM.	26789553
BA/F3	Function assay		72 hrs	Inhibition of BCR/ABL p210-Q252H mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=0.659μM.	26789553
BA/F3	Function assay		72 hrs	Inhibition of BCR/ABL p210-F317I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=0.855μM.	26789553
BA/F3	Function assay		72 hrs	Inhibition of BCR/ABL p210-H369P mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=1.69μM.	26789553
BA/F3	Function assay		72 hrs	Inhibition of BCR/ABL p210-E255K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=1.93μM.	26789553
BA/F3	Function assay		72 hrs	Inhibition of TEL-SRC (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=2.1μM.	26789553
BA/F3	Function assay		72 hrs	Inhibition of BCR/ABL p210-F317L mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=2.169μM.	26789553
BA/F3	Function assay		72 hrs	Inhibition of TEL-DDR1 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=3μM.	26789553
BA/F3	Function assay		72 hrs	Inhibition of TEL-BLK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=4.1μM.	26789553
HEL	Antiproliferative assay		72 hrs	Antiproliferative activity against human HEL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=5.3μM.	26789553
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=6.7μM.	26789553
BA/F3	Function assay		72 hrs	Inhibition of TEL-DDR2 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=7.7μM.	26789553
BA/F3	Function assay		72 hrs	Inhibition of TEL-HCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=9.7μM.	26789553
K562	Cytotoxicity assay		72 hrs	Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay, IC50=0.51μM.	26814890
K562/G	Cytotoxicity assay		72 hrs	Cytotoxicity against human K562/G cells assessed as cell viability after 72 hrs by MTT assay, IC50=4.65μM.	26814890
BA/F3	Function assay		48 hrs	Inhibition of imatinib-resistant PDGFR D842V mutant (unknown origin) expressed in mouse BA/F3 cells assessed as decrease in cell viability after 48 hrs by CellTiter 96 aqueous one solution cell proliferation assay, IC50=0.642μM.	26844689
HL60	Antiproliferative assay		72 hrs	Antiproliferative activity against human HL60 cells assessed as inhibition of cell survival after 72 hrs by MTT assay, IC50=0.03μM.	26850004
K562	Antiproliferative assay		72 hrs	Antiproliferative activity against human K562 cells assessed as inhibition of cell survival after 72 hrs by MTT assay, IC50=0.38μM.	26850004
KG1a	Antiproliferative assay		72 hrs	Antiproliferative activity against human KG1a cells assessed as inhibition of cell survival after 72 hrs by MTT assay, IC50=16.7μM.	26850004
BAF3	Function assay		72 hrs	Inhibition of human wild type BCR-ABL expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, EC50=0.034μM.	27010810
JURL-MK1	Antiproliferative assay		48 hrs	Antiproliferative activity against human JURL-MK1 cells after 48 hrs by Cell-Titer-Glo luminescent cell viability assay, GI50=0.06μM.	27011159
BV173	Antiproliferative assay		48 hrs	Antiproliferative activity against human BV173 cells after 48 hrs by Cell-Titer-Glo luminescent cell viability assay, GI50=0.1μM.	27011159
K562	Antiproliferative assay		48 hrs	Antiproliferative activity against human K562 cells after 48 hrs by Cell-Titer-Glo luminescent cell viability assay, GI50=0.2μM.	27011159
EM2	Antiproliferative assay		48 hrs	Antiproliferative activity against human EM2 cells after 48 hrs by Cell-Titer-Glo luminescent cell viability assay, GI50=0.26μM.	27011159
KCL22	Antiproliferative assay		48 hrs	Antiproliferative activity against human KCL22 cells after 48 hrs by Cell-Titer-Glo luminescent cell viability assay, GI50=0.43μM.	27011159
GISTT1	Antiproliferative assay		72 hrs	Antiproliferative activity against cKIT dependent human GISTT1 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50=0.008μM.	27077705
GIST882	Antiproliferative assay		72 hrs	Antiproliferative activity against cKIT dependent human GIST882 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50=0.014μM.	27077705
BAF3	Function assay		72 hrs	Inhibition of Tel-fused cKIT V559D mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50=0.039μM.	27077705
MEG01	Antiproliferative assay		72 hrs	Antiproliferative activity against human BCR-ABL dependent MEG01 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50=0.074μM.	27077705
BAF3	Function assay		72 hrs	Inhibition of Tel-fused cKIT L567P mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50=0.1μM.	27077705
K562	Antiproliferative assay		72 hrs	Antiproliferative activity against BCR-ABL dependent human K562 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50=0.12μM.	27077705
KU812	Antiproliferative assay		72 hrs	Antiproliferative activity against BCR-ABL dependent human KU812 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50=0.16μM.	27077705
BAF3	Function assay		72 hrs	Inhibition of Tel-fused cKIT (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50=0.4μM.	27077705
BAF3	Function assay		72 hrs	Inhibition of Tel-fused cKIT N822K mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50=1.29μM.	27077705
BAF3	Function assay		72 hrs	Inhibition of Tel-fused cKIT V654A mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50=2.49μM.	27077705
BAF3	Function assay		72 hrs	Inhibition of Tel-fused cKIT V559D/V654A double mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50=3μM.	27077705
BAF3	Function assay		72 hrs	Inhibition of Tel-fused cKIT T670I/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50=6.67μM.	27077705
K562	Cytotoxicity assay		72 hrs	Cytotoxicity against human K562 cells assessed as decrease in cell proliferation after 72 hrs by XTT assay, IC50=0.31μM.	27214512
A10	Function assay		68 hrs	Inhibition of PDGFR-beta driven proliferation of rat A10 cells after 68 hrs in presence of rat recombinant PDGF-BB by cell titer-glo luminescence assay, IC50=0.162μM.	27502700
BA/F3	Function assay		72 hrs	Inhibition of TEL-fused cKIT L567P mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.01μM.	27545040
GIST-T1	Function assay		72 hrs	Inhibition of wild type cKIT in human GIST-T1 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.027μM.	27545040
Sf9	Function assay		1 hr	Inhibition of His-tagged cKIT (unknown origin) expressed in Sf9 cells using Poly(4:1 Glu, Tyr) peptide as substrate after 1 hr by ADP-glo kinase assay, IC50=0.319μM.	27545040
BA/F3	Function assay		72 hrs	Inhibition of TEL-fused cKIT N822K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.36μM.	27545040
BA/F3	Function assay		72 hrs	Inhibition of TEL-fused cKIT (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.59μM.	27545040
BA/F3	Function assay		72 hrs	Inhibition of TEL-fused cKIT V654A mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.7μM.	27545040
BA/F3	Function assay		72 hrs	Inhibition of TEL-fused cKIT V559D/V654A double mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.7μM.	27545040
BA/F3	Function assay		72 hrs	Inhibition of TEL-fused cKIT T670I/V559D double mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=5.2μM.	27545040
GIST-5R	Function assay		72 hrs	Inhibition of wild type cKIT T670I mutant in human GIST-5R cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=8.3μM.	27545040
BA/F3	Function assay		72 hrs	Inhibition of TEL-fused cKIT T670I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=9.6μM.	27545040
Sf9	Function assay		1 hr	Inhibition of His-tagged cKIT T670I mutant (544 to 935 residues) (unknown origin) expressed in Sf9 cells using Poly(4:1 Glu, Tyr) peptide as substrate after 1 hr by ADP-glo kinase assay, IC50=9.818μM.	27545040
GISTT1	Antiproliferative assay		72 hrs	Antiproliferative activity against human GISTT1 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.008μM.	27966954
GIST882	Antiproliferative assay		72 hrs	Antiproliferative activity against human GIST882 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.014μM.	27966954
BAF3	Function assay		72 hrs	Inhibition of Tel-fused PDGFR-beta (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.019μM.	27966954
BAF3	Function assay		72 hrs	Inhibition of Tel-fused PDGFR-alpha (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.034μM.	27966954
BAF3	Function assay		72 hrs	Inhibition of Tel-fused c-KIT V559D mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.039μM.	27966954
MEG01	Antiproliferative assay		72 hrs	Antiproliferative activity against human MEG01 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.074μM.	27966954
BAF3	Function assay		72 hrs	Inhibition of Tel-fused c-KIT L576P mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.102μM.	27966954
BAF3	Function assay		72 hrs	Inhibition of Tel-fused CSF1R (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.11μM.	27966954
KU812	Antiproliferative assay		72 hrs	Antiproliferative activity against human KU812 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.163μM.	27966954
SF9	Function assay		1 hr	Inhibition of C-terminal His-tagged human ABL1 expressed in baculovirus infected SF9 cells using Tyr 02 peptide as substrate measured after 1 hr by FRET based Z'Lyte assay, IC50=0.223μM.	27966954
K562	Antiproliferative assay		72 hrs	Antiproliferative activity against human K562 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.267μM.	27966954
BAF3	Function assay		72 hrs	Inhibition of human BCR/ABL p210 fusion protein expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.27μM.	27966954
BAF3	Function assay		72 hrs	Inhibition of Tel-fused c-KIT (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.37μM.	27966954
BAF3	Function assay		72 hrs	Inhibition of BCR/ABL p210 fusion protein M356T mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.625μM.	27966954
BAF3	Function assay		72 hrs	Inhibition of BCR/ABL p210 fusion protein F317I mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=0.85μM.	27966954
BAF3	Function assay		72 hrs	Inhibition of Tel-fused c-KIT N822K mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=1.29μM.	27966954
BAF3	Function assay		72 hrs	Inhibition of BCR/ABL p210 fusion protein H369P mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=1.79μM.	27966954
BAF3	Function assay		72 hrs	Inhibition of BCR/ABL p210 fusion protein F317L mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=2.16μM.	27966954
BAF3	Function assay		72 hrs	Inhibition of Tel-fused c-KIT V654A mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=2.49μM.	27966954
BAF3	Function assay		72 hrs	Inhibition of Tel-fused c-KIT V559D/V654A double mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=3μM.	27966954
BAF3	Function assay		72 hrs	Inhibition of Tel-fused c-KIT T670I mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50=6.67μM.	27966954
K562	Function assay		30 mins	Inhibition of kinobead binding to NQO2 in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method, IC50=0.043μM.	28280261
K562	Function assay		30 mins	Inhibition of kinobead binding to DDR1 in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method, IC50=0.09μM.	28280261
K562	Function assay		30 mins	Inhibition of kinobead binding to ABL in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method, IC50=0.25μM.	28280261
K562	Function assay		30 mins	Inhibition of kinobead binding to ARG in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method, IC50=0.272μM.	28280261
K562	Antiproliferative assay		48 hrs	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50=0.53μM.	28525838
A549	Antiproliferative assay		48 hrs	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50=4.56μM.	28525838
GISTT1	Antiproliferative assay		72 hrs	Antiproliferative activity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.003μM.	28541695
BAF3	Function assay		72 hrs	Inhibition of TEL-fused PDGFRalpha (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.0107μM.	28541695
GIST882	Antiproliferative assay		72 hrs	Antiproliferative activity against human GIST882 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.02μM.	28541695
BAF3	Function assay		72 hrs	Inhibition of TEL-fused cKIT C674S mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.0249μM.	28541695
BAF3	Function assay		72 hrs	Inhibition of TEL-fused cKIT V559D mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.036μM.	28541695
MEG01	Antiproliferative assay		72 hrs	Antiproliferative activity against human MEG01 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.045μM.	28541695
BAF3	Function assay		72 hrs	Inhibition of TEL-fused cKIT L576P mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.0451μM.	28541695
KU812	Antiproliferative assay		72 hrs	Antiproliferative activity against human KU812 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.11μM.	28541695
K562	Antiproliferative assay		72 hrs	Antiproliferative activity against human K562 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.147μM.	28541695
BAF3	Function assay		72 hrs	Inhibition of TEL-fused cKIT A829P mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.1482μM.	28541695
BAF3	Function assay		72 hrs	Inhibition of TEL-fused cKIT (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.3819μM.	28541695
BAF3	Function assay		72 hrs	Inhibition of TEL-fused cKIT V559D/V654A double mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.803μM.	28541695
BAF3	Function assay		72 hrs	Inhibition of TEL-fused cKIT V654A mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=0.8031μM.	28541695
BAF3	Function assay		72 hrs	Inhibition of TEL-fused cKIT D816H mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=1.245μM.	28541695
BAF3	Function assay		72 hrs	Inhibition of TEL-fused cKIT N822K mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=1.466μM.	28541695
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=4.686μM.	28541695
GIST48B	Antiproliferative assay		72 hrs	Antiproliferative activity against human GIST48B cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50=6.986μM.	28541695
BAF3	Function assay		72 hrs	Inhibition of ABL in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=0.73μM.	28974338
BAF3	Function assay		72 hrs	Inhibition of ABL T315I mutant in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=20.03μM.	28974338
GISTT1	Cytotoxicity assay		72 hrs	Cytotoxicity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50=0.04μM.	28991465
GIST430	Cytotoxicity assay		72 hrs	Cytotoxicity against human GIST430 cells harboring KIT V654A mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50=1.1μM.	28991465
EOL-1	Antiproliferative assay		72 hrs	Antiproliferative activity against human EOL-1 cells after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50<0.001μM.	29544149
BA/F3	Function assay		72 hrs	Inhibition of TEL-fused PDGFRbeta (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=0.019μM.	29544149
BA/F3	Function assay		72 hrs	Inhibition of TEL-fused PDGFRalpha (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=0.034μM.	29544149
NCI-H1703	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1703 cells after 72 hrs in presence of PDGF-AA by CellTiter-Glo or CCK-8 assay, GI50=0.23μM.	29544149
BA/F3	Function assay		72 hrs	Inhibition of TEL-fused c-KIT (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=0.37μM.	29544149
NCI-H1703	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1703 cells after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50=2.1μM.	29544149
K562	Cytotoxicity assay		48 hrs	Cytotoxicity in drug sensitive human K562 cells assessed as reduction cell viability incubated for 48 hrs by XTT assay, IC50=1.1μM.	29655981
K562	Antiproliferative assay		72 hrs	Antiproliferative activity against human K562 cells after 72 hrs by MTT assay, IC50=3.43μM.	29684708
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50=7.12μM.	29684708
A2780	Antiproliferative assay		72 hrs	Antiproliferative activity against human A2780 cells after 72 hrs by MTT assay, IC50=8.9μM.	29684708
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50=19.66μM.	29684708
HT-29	Antiproliferative assay		96 hrs	Antiproliferative activity against human HT-29 cells after 96 hrs by SRB assay, IC50=0.06μM.	29724653
GIST882	Antiproliferative assay		96 hrs	Antiproliferative activity against imatinib-susceptible human GIST882 cells harboring c-KIT K642E mutant after 96 hrs by SRB assay, IC50=1.7μM.	29724653
HGC27	Antiproliferative assay		96 hrs	Antiproliferative activity against human HGC27 cells after 96 hrs by SRB assay, IC50=2.4μM.	29724653
MCF7	Antiproliferative assay		96 hrs	Antiproliferative activity against human MCF7 cells after 96 hrs by SRB assay, IC50=11.3μM.	29724653
GIST48	Antiproliferative assay		96 hrs	Antiproliferative activity against imatinib-resistant human GIST48 cells harboring c-KIT V560D/D820A double mutant after 96 hrs by SRB assay, IC50=19.8μM.	29724653
Ba/F3	Function assay		48 hrs	Inhibition of BCR-ABL1 G250H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50=0.0771μM.	30137981
Ba/F3	Function assay		48 hrs	Inhibition of wild type BCR-ABL1 (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay, GI50=0.0905μM.	30137981
Ba/F3	Function assay		48 hrs	Inhibition of BCR-ABL1 E355G mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50=0.149μM.	30137981
Ba/F3	Function assay		48 hrs	Inhibition of BCR-ABL1 E459K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50=0.201μM.	30137981
Ba/F3	Function assay		48 hrs	Inhibition of BCR-ABL1 F359V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50=0.249μM.	30137981
Ba/F3	Function assay		48 hrs	Inhibition of BCR-ABL1 Q252H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50=0.455μM.	30137981
Ba/F3	Function assay		48 hrs	Inhibition of BCR-ABL1 Y253H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50=0.836μM.	30137981
Ba/F3	Function assay		48 hrs	Inhibition of BCR-ABL1 E255K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50=0.838μM.	30137981
Ba/F3	Function assay		48 hrs	Inhibition of BCR-ABL1 E255V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50=0.874μM.	30137981
Ba/F3	Function assay		48 hrs	Inhibition of BCR-ABL1 T315I mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay, GI50=9.645μM.	30137981
BA/F3	Function assay		72 hrs	Inhibition of Kit exon 11 deletion (557 to 558 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.017μM.	30204441
BA/F3	Function assay		72 hrs	Inhibition of TEL-fused PDGFRalpha (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.046μM.	30204441
BA/F3	Function assay		72 hrs	Inhibition of Kit V560D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.07μM.	30204441
BA/F3	Function assay		72 hrs	Inhibition of TEL-fused PDGFRbeta (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.102μM.	30204441
BA/F3	Function assay		72 hrs	Inhibition of Kit exon 9 AY502 to 503 insertion mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.192μM.	30204441
BA/F3	Function assay		72 hrs	Inhibition of Kit exon 11 deletion (557 to 558 residues) and D820A mutant and D820A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.216μM.	30204441
BA/F3	Function assay		72 hrs	Inhibition of Kit exon 11 deletion (557 to 558 residues) and N822K mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.223μM.	30204441
BA/F3	Function assay		72 hrs	Inhibition of Kit exon 11 deletion (557 to 558 residues) and A829P mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.312μM.	30204441
BA/F3	Function assay		72 hrs	Inhibition of Kit exon 11 deletion (557 to 558 residues) and V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.392μM.	30204441
BA/F3	Function assay		72 hrs	Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.535μM.	30204441
BA/F3	Function assay		72 hrs	Inhibition of PDGFRalpha V561D/D842V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.567μM.	30204441
BA/F3	Function assay		72 hrs	Inhibition of Kit exon 11 deletion (557 to 558 residues) and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.669μM.	30204441
BA/F3	Function assay		72 hrs	Inhibition of Kit V560D/V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=0.701μM.	30204441
BA/F3	Function assay		72 hrs	Inhibition of Kit V560D/D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=1.191μM.	30204441
BA/F3	Function assay		72 hrs	Inhibition of Kit exon 11 deletion (560 to 578 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=1.523μM.	30204441
BA/F3	Function assay		72 hrs	Inhibition of Kit exon 9 AY502 to 503 insertion and D816 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=2.749μM.	30204441
BA/F3	Function assay		72 hrs	Inhibition of Kit exon 9 AY502 to 503 insertion and V654 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=3.947μM.	30204441
BA/F3	Function assay		72 hrs	Inhibition of Kit D816V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50=9.93μM.	30204441
K562	Cytotoxicity assay		24 hrs	Cytotoxicity against imatinib-sensitive human K562 cells assessed as decrease in cell viability after 24 hrs by XTT assay, IC50=1μM.	30261468
Sf9	Function assay		60 mins	Inhibition of inactive wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8 hrs by ADP-G, IC50=0.043μM.	30317026
K562	Antiproliferative assay		72 hrs	Antiproliferative activity in human K562 cells after 72 hrs by CCK8 assay, GI50=0.25μM.	30317026
BAF3	Function assay		72 hrs	Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.26μM.	30317026
MEG01	Antiproliferative assay		72 hrs	Antiproliferative activity in human MEG01 cells after 72 hrs by CCK8 assay, GI50=0.28μM.	30317026
BAF3	Function assay		72 hrs	Inhibition of wild type BCR/ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.29μM.	30317026
KU812	Antiproliferative assay		72 hrs	Antiproliferative activity in human KU812 cells after 72 hrs by CCK8 assay, GI50=0.31μM.	30317026
BAF3	Function assay		72 hrs	Inhibition of BCR/ABL V299L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.65μM.	30317026
BAF3	Function assay		72 hrs	Inhibition of BCR/ABL M351T mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.85μM.	30317026
BAF3	Function assay		72 hrs	Inhibition of BCR/ABL F317I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.95μM.	30317026
BAF3	Function assay		72 hrs	Inhibition of BCR/ABL Q252H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=1.17μM.	30317026
Sf9	Function assay		1 hr	Inhibition of active wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay, IC50=1.5μM.	30317026
BAF3	Function assay		72 hrs	Inhibition of BCR/ABL F317L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=2.24μM.	30317026
BAF3	Function assay		72 hrs	Inhibition of BCR/ABL H369P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=3.75μM.	30317026
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay, IC50=44.55μM.	30562697
K562	Antiproliferative assay		72 hrs	Antiproliferative activity against human K562 cells after 72 hrs by MTT assay, IC50=0.00015μM.	30605831
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay, IC50=6.33μM.	30798049
MDA-MB-453	Cytotoxicity assay		48 hrs	Cytotoxicity against human MDA-MB-453 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay, IC50=12.84μM.	30798049
BAF3	Function assay		72 hrs	Inhibition of TEL fused c-KIT V559G mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.001μM.	31046271
BAF3	Function assay		72 hrs	Inhibition of TEL fused c-KIT V559A mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.005μM.	31046271
GISTT1	Antiproliferative assay		72 hrs	Antiproliferative activity against human GISTT1 cells harboring c-KIT 560 to 578 deletion mutant incubated for 72 hrs by CCK8 assay, GI50=0.026μM.	31046271
BAF3	Function assay		72 hrs	Inhibition of TEL fused c-KIT V559D mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.039μM.	31046271
GIST882	Antiproliferative assay		72 hrs	Antiproliferative activity against human GIST882 cells harboring c-KIT K642E mutant incubated for 72 hrs by CCK8 assay, GI50=0.058μM.	31046271
BAF3	Function assay		72 hrs	Inhibition of TEL fused c-KIT L576P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.115μM.	31046271
BAF3	Function assay		72 hrs	Inhibition of TEL fused c-KIT D820E mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.267μM.	31046271
BAF3	Function assay		72 hrs	Inhibition of wild type TEL fused c-KIT (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.364μM.	31046271
BAF3	Function assay		72 hrs	Inhibition of TEL fused c-KIT A829P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.406μM.	31046271
BAF3	Function assay		72 hrs	Inhibition of TEL fused c-KIT D816H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.823μM.	31046271
BAF3	Function assay		72 hrs	Inhibition of TEL fused c-KIT N822K mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=1.29μM.	31046271
BAF3	Function assay		72 hrs	Inhibition of TEL fused c-KIT V654A/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=1.57μM.	31046271
BAF3	Function assay		72 hrs	Inhibition of TEL fused c-KIT V654A mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=2.3μM.	31046271
K562	Antiproliferative assay		72 hrs	Antiproliferative activity against human K562 cells assessed as inhibition of cell viability incubated for 72 hrs by real time live-cell imaging technique, IC50=0.14μM.	31097376
K562	Antiproliferative assay		48 hrs	Antiproliferative activity against human BCR/ABL positive K562 cells assessed as growth inhibition measured after 48 hrs by MTT assay, IC50=4.26μM.	31185413
BAF3	Function assay		72 hrs	Inhibition of c-KIT V560D mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.003μM.	31250638
BAF3	Function assay		72 hrs	Inhibition of c-KIT V559G mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.008μM.	31250638
BAF3	Function assay		72 hrs	Inhibition of c-KIT V559D mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.01μM.	31250638
GISTT1	Function assay		72 hrs	Inhibition of c-KIT 560 to 578 deletion mutant in human GISTT1 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.015μM.	31250638
BAF3	Function assay		72 hrs	Inhibition of c-KIT D820E mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.035μM.	31250638
GIST882	Function assay		72 hrs	Inhibition of c-KIT K642E mutant in human GIST882 cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.048μM.	31250638
BAF3	Function assay		72 hrs	Inhibition of c-KIT L576P mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.085μM.	31250638
BAF3	Function assay		72 hrs	Inhibition of c-KIT S709F mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.115μM.	31250638
BAF3	Function assay		72 hrs	Inhibition of c-KIT D816E mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.174μM.	31250638
BAF3	Function assay		72 hrs	Inhibition of c-KIT D820G mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.337μM.	31250638
BAF3	Function assay		72 hrs	Inhibition of c-KIT in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.35μM.	31250638
BAF3	Function assay		72 hrs	Inhibition of c-KIT D820Y mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.435μM.	31250638
BAF3	Function assay		72 hrs	Inhibition of c-KIT A829P mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.58μM.	31250638
BAF3	Function assay		72 hrs	Inhibition of c-KIT V654A/V559D double mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.608μM.	31250638
BAF3	Function assay		72 hrs	Inhibition of c-KIT D816H mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.651μM.	31250638
BAF3	Function assay		72 hrs	Inhibition of c-KIT V559A mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=0.905μM.	31250638
BAF3	Function assay		72 hrs	Inhibition of c-KIT V654A mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=1.41μM.	31250638
BAF3	Function assay		72 hrs	Inhibition of c-KIT N822K mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=1.47μM.	31250638
BAF3	Function assay		72 hrs	Inhibition of c-KIT T670E mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=4.08μM.	31250638
BAF3	Function assay		72 hrs	Inhibition of c-KIT Y823D mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay, GI50=5.87μM.	31250638
GISTT1	Antiproliferative assay		72 hrs	Antiproliferative activity against human GISTT1 cells harboring c-KIT 560 to 578 deletion mutant measured after 72 hrs by CCK8 assay	31250638
EOL-1	Cytotoxicity assay		72 hrs	Cytotoxicity against FIP1L1-PDGFRA positive human EOL-1 cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis, GI50<0.0005μM.	31514019
K562	Cytotoxicity assay		72 hrs	Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis, GI50=0.73μM.	31514019
CEM	Cytotoxicity assay		72 hrs	Cytotoxicity against human CEM cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis, GI50=35.809μM.	31514019
Ba/F3	Function assay		72 hrs	Inhibition of wild type BCR/Abl (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=0.1438μM.	31699612
Ba/F3	Function assay		72 hrs	Inhibition of BCR/Abl P230 mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=0.2215μM.	31699612
Ba/F3	Function assay		72 hrs	Inhibition of BCR/Abl P190 mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=0.3455μM.	31699612
Ba/F3	Function assay		72 hrs	Inhibition of BCR/Abl F317I mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=0.364μM.	31699612
Ba/F3	Function assay		72 hrs	Inhibition of BCR/Abl V299L mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=0.4053μM.	31699612
Ba/F3	Function assay		72 hrs	Inhibition of BCR/Abl Q252H mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=0.4865μM.	31699612
Ba/F3	Function assay		72 hrs	Inhibition of BCR/Abl F317L mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=0.7163μM.	31699612
Ba/F3	Function assay		72 hrs	Inhibition of BCR/Abl M351T mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=0.7993μM.	31699612
Ba/F3	Function assay		72 hrs	Inhibition of BCR/Abl H396P mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=2.706μM.	31699612
Ba/F3	Function assay		72 hrs	Inhibition of BCR/Abl E255K mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=3.257μM.	31699612
Ba/F3	Function assay		72 hrs	Inhibition of BCR/Abl Y253F mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=8.778μM.	31699612
GISTT1	Antiproliferative assay		72 hrs	Antiproliferative activity against human GISTT1 cells harboring heterozygous deletion mutation at C-kit exon 11 assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay, GI50=0.04μM.	31721578
Sf9	Function assay		150 mins	Inhibition of recombinant N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) (unknown origin) expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr) 4:1 as substrate measured after 150 mins in presence of , IC50=0.053μM.	31721578
Sf9	Function assay		4 hrs	Inhibition of wild type recombinant GST-tagged FLT3 (Y567 to S993 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using Her2 peptide as substrate measured after 4 hrs in presence of ATP by Kinase-Glo Plus reagent-based lumine, IC50=0.131μM.	31721578
GIST882	Antiproliferative assay		144 hrs	Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as cell growth inhibition after 144 hrs by methylene blue staining based assay, GI50=0.195μM.	31721578
GIST430	Antiproliferative assay		120 hrs	Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as cell growth inhibition after 120 hrs by methylene blue staining , GI50=0.625μM.	31721578
GIST48	Antiproliferative assay		120 hrs	Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as cell growth inhibition after 120 hrs by methylene blue staining based assay, GI50=0.929μM.	31721578
CTV-1	Growth Inhibition Assay			IC50=33.9789 μM	SANGER
Calu-6	Growth Inhibition Assay			IC50=33.1855 μM	SANGER
EW-1	Growth Inhibition Assay			IC50=32.9454 μM	SANGER
NTERA-S-cl-D1	Growth Inhibition Assay			IC50=30.5093 μM	SANGER
ES1	Growth Inhibition Assay			IC50=27.521 μM	SANGER
L-540	Growth Inhibition Assay			IC50=26.9143 μM	SANGER
LS-513	Growth Inhibition Assay			IC50=26.8847 μM	SANGER
NB10	Growth Inhibition Assay			IC50=26.4699 μM	SANGER
MPP-89	Growth Inhibition Assay			IC50=25.6874 μM	SANGER
DMS-79	Growth Inhibition Assay			IC50=24.4934 μM	SANGER
GDM-1	Growth Inhibition Assay			IC50=22.5945 μM	SANGER
ALL-PO	Growth Inhibition Assay			IC50=20.8149 μM	SANGER
RS4-11	Growth Inhibition Assay			IC50=20.3308 μM	SANGER
SCLC-21H	Growth Inhibition Assay			IC50=20.1246 μM	SANGER
NKM-1	Growth Inhibition Assay			IC50=19.3552 μM	SANGER
LB1047-RCC	Growth Inhibition Assay			IC50=18.4452 μM	SANGER
KARPAS-45	Growth Inhibition Assay			IC50=18.1848 μM	SANGER
LC4-1	Growth Inhibition Assay			IC50=18.0652 μM	SANGER
HH	Growth Inhibition Assay			IC50=17.3999 μM	SANGER
TE-441-T	Growth Inhibition Assay			IC50=17.2886 μM	SANGER
NCI-H510A	Growth Inhibition Assay			IC50=17.2442 μM	SANGER
LB2518-MEL	Growth Inhibition Assay			IC50=16.6094 μM	SANGER
ES7	Growth Inhibition Assay			IC50=14.7379 μM	SANGER
BB49-HNC	Growth Inhibition Assay			IC50=14.3335 μM	SANGER
SCC-15	Growth Inhibition Assay			IC50=10.7788 μM	SANGER
TGBC24TKB	Growth Inhibition Assay			IC50=8.34052 μM	SANGER
LB2241-RCC	Growth Inhibition Assay			IC50=8.07384 μM	SANGER
IMR-5	Growth Inhibition Assay			IC50=6.22147 μM	SANGER
NCI-H1770	Growth Inhibition Assay			IC50=5.57262 μM	SANGER
SUP-T1	Growth Inhibition Assay			IC50=3.82907 μM	SANGER
BE-13	Growth Inhibition Assay			IC50=2.62106 μM	SANGER
A498	Growth Inhibition Assay			IC50=2.57223 μM	SANGER
NOS-1	Growth Inhibition Assay			IC50=1.65383 μM	SANGER
NCI-H1436	Growth Inhibition Assay			IC50=0.97801 μM	SANGER
ST486	Growth Inhibition Assay			IC50=0.6854 μM	SANGER
CGTH-W-1	Growth Inhibition Assay			IC50=0.38374 μM	SANGER
K-562	Growth Inhibition Assay			IC50=0.22432 μM	SANGER
BV-173	Growth Inhibition Assay			IC50=0.1874 μM	SANGER
MEG-01	Growth Inhibition Assay			IC50=0.08921 μM	SANGER
EM-2	Growth Inhibition Assay			IC50=0.0888 μM	SANGER
LAMA-84	Growth Inhibition Assay			IC50=0.07304 μM	SANGER
YT	Growth Inhibition Assay			IC50=38.5209 μM	SANGER
TE-6	Growth Inhibition Assay			IC50=41.2798 μM	SANGER
HT-144	Growth Inhibition Assay			IC50=41.5486 μM	SANGER
EW-13	Growth Inhibition Assay			IC50=42.2791 μM	SANGER
KALS-1	Growth Inhibition Assay			IC50=43.1329 μM	SANGER
MOLT-16	Growth Inhibition Assay			IC50=45.0752 μM	SANGER
D-336MG	Growth Inhibition Assay			IC50=45.9599 μM	SANGER
TE-11	Growth Inhibition Assay			IC50=46.653 μM	SANGER
EB2	Growth Inhibition Assay			IC50=46.699 μM	SANGER
SK-N-DZ	Growth Inhibition Assay			IC50=48.0961 μM	SANGER
SW684	Growth Inhibition Assay			IC50=48.2695 μM	SANGER
EW-18	Growth Inhibition Assay			IC50=48.4395 μM	SANGER
RL95-2	Growth Inhibition Assay			IC50=50.071 μM	SANGER
CHP-126	Growth Inhibition Assay			IC50=50.8905 μM	SANGER
NCI-H1395	Growth Inhibition Assay			IC50=51.7835 μM	SANGER
TE-15	Growth Inhibition Assay			IC50=52.2556 μM	SANGER
ES4	Growth Inhibition Assay			IC50=52.9775 μM	SANGER
TE-1	Growth Inhibition Assay			IC50=53.9455 μM	SANGER
SIMA	Growth Inhibition Assay			IC50=57.3311 μM	SANGER
LB647-SCLC	Growth Inhibition Assay			IC50=64.1188 μM	SANGER
KY821	Growth Inhibition Assay			IC50=64.2552 μM	SANGER
LC-2-ad	Growth Inhibition Assay			IC50=65.7601 μM	SANGER
KP-N-RT-BM-1	Growth Inhibition Assay			IC50=66.6366 μM	SANGER
SW872	Growth Inhibition Assay			IC50=67.4382 μM	SANGER
ES5	Growth Inhibition Assay			IC50=67.6968 μM	SANGER
SK-NEP-1	Growth Inhibition Assay			IC50=68.3803 μM	SANGER
RPMI-6666	Growth Inhibition Assay			IC50=71.032 μM	SANGER
UACC-812	Growth Inhibition Assay			IC50=71.1609 μM	SANGER
COLO-829	Growth Inhibition Assay			IC50=72.6987 μM	SANGER
KP-N-YS	Growth Inhibition Assay			IC50=72.7139 μM	SANGER
GI-1	Growth Inhibition Assay			IC50=73.2868 μM	SANGER
ETK-1	Growth Inhibition Assay			IC50=73.4932 μM	SANGER
LXF-289	Growth Inhibition Assay			IC50=73.729 μM	SANGER
CAS-1	Growth Inhibition Assay			IC50=73.8857 μM	SANGER
EW-22	Growth Inhibition Assay			IC50=74.7115 μM	SANGER
NCI-H2196	Growth Inhibition Assay			IC50=75.6379 μM	SANGER
EoL-1-cell	Growth Inhibition Assay			IC50=81.6963 μM	SANGER
D-247MG	Growth Inhibition Assay			IC50=82.0248 μM	SANGER
Becker	Growth Inhibition Assay			IC50=82.3481 μM	SANGER
IST-MEL1	Growth Inhibition Assay			IC50=82.3482 μM	SANGER
MDA-MB-134-VI	Growth Inhibition Assay			IC50=82.5996 μM	SANGER
NCI-H1092	Growth Inhibition Assay			IC50=84.0197 μM	SANGER
KINGS-1	Growth Inhibition Assay			IC50=86.1618 μM	SANGER
HCC2218	Growth Inhibition Assay			IC50=86.7913 μM	SANGER
GI-ME-N	Growth Inhibition Assay			IC50=87.7699 μM	SANGER
AM-38	Growth Inhibition Assay			IC50=88.3953 μM	SANGER
KNS-42	Growth Inhibition Assay			IC50=89.1018 μM	SANGER
C8166	Growth Inhibition Assay			IC50=89.6125 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay			IC50=89.8719 μM	SANGER
CTB-1	Growth Inhibition Assay			IC50=90.6357 μM	SANGER
HCE-4	Growth Inhibition Assay			IC50=91.1336 μM	SANGER
NCI-H526	Growth Inhibition Assay			IC50=92.4103 μM	SANGER
ECC4	Growth Inhibition Assay			IC50=94.2555 μM	SANGER
NCCIT	Growth Inhibition Assay			IC50=95.3292 μM	SANGER
MZ7-mel	Growth Inhibition Assay			IC50=95.904 μM	SANGER
COLO-684	Growth Inhibition Assay			IC50=96.2385 μM	SANGER
SU-DHL-1	Growth Inhibition Assay			IC50=96.9842 μM	SANGER
SF126	Growth Inhibition Assay			IC50=97.5217 μM	SANGER
NMC-G1	Growth Inhibition Assay			IC50=98.4554 μM	SANGER
NB14	Growth Inhibition Assay			IC50=98.9208 μM	SANGER
VA-ES-BJ	Growth Inhibition Assay			IC50=99.4056 μM	SANGER
CHO	Function assay			Inhibition of wild type Platelet-derived growth factor receptor beta phosphorylation in CHO cells, IC50=0.24μM.	12166950
CHO	Function assay			Inhibition of chimeric PDGF receptor with c-kit cytoplasmic domain phosphorylation in CHO cells, IC50=0.26μM.	12166950
CHO	Function assay			Inhibition of chimeric PDGF receptor with CSF-1R cytoplasmic domain phosphorylation in CHO cells, IC50=0.96μM.	12166950
K562	Cytotoxicity assay			Cytotoxic effect in K562 cells, IC50=0.11μM.	12951113
K562	Function assay			Inhibitory activity against human K562 cells growth using MTT assay, IC50=0.4μM.	14552760
Sf9	Function assay			TP_TRANSPORTER: inhibition of ATPase activity in BCRP-expressing Sf9 cells, IC50=0.5μM.	15155841
Sf9	Function assay			TP_TRANSPORTER: efflux of Hoechst33342 in BCRP-expressing Sf9 cells, IC50=0.9μM.	15155841
K562	Antiproliferative assay			Antiproliferative activity against K562 cells, IC50=0.182μM.	16332440
U937	Antiproliferative assay			Antiproliferative activity against U937 cells, IC50=14μM.	16332440
32D	Cytotoxicity assay			Cytotoxic activity against mouse 32D cells transfected with p210 Bcr-abl, IC50=0.19μM.	16415863
32D	Cytotoxicity assay			Cytotoxic activity against mouse 32D Bcr-abl negative cells, IC50=20μM.	16415863
BaF3	Antiproliferative assay			Antiproliferative activity against murine BaF3 cells expressing wild type NPM/ALK by [3H]thymidine uptake assay, IC50=7.1μM.	16970400
BaF3	Antiproliferative assay			Antiproliferative activity against murine BaF3 cells expressing NPM/ALK L256T mutant by [3H]thymidine uptake assay, IC50=9.1μM.	16970400
Sf9	Function assay			Inhibition of human Lyn kinase expressed in Sf9 cells, IC50=0.22μM.	17376680
Sf9	Function assay			Inhibition of human Abl kinase expressed in Sf9 cells, IC50=0.47μM.	17376680
K562	Cytotoxicity assay			Cytotoxicity against K562 cells by MTT assay, IC50=0.18μM.	17572088
A2780/ADR	Function assay			Inhibition of P-glycoprotein expressed in A2780/ADR cells by calcein AM assay, IC50=7.24436μM.	17890094
MO7e	Function assay			Inhibition of SCF-induced phosphorylation of c-Kit in MO7e cells by TR-FRET assay, IC50=0.046μM.	18447379
MCF7	Function assay			Inhibition of ABCG2 in human mitoxantrone-resistant MCF7 cells by Hoechst 33342 assay, IC50=4.89779μM.	18678495
A2780	Function assay			Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay, IC50=7.24436μM.	18678495
CML	Antiproliferative assay			Antiproliferative activity against human CML cells, IC50=0.35μM.	19219016
ALL3	Cytotoxicity assay			Cytotoxicity against Philadelphia chromosome positive human ALL3 cells by Alamar Blue fluorescent assay, IC50=0.333μM.	19889540
MDCK	Function assay			Inhibition of BCRP expressed in MDCK cells by pheophorbide A assay, IC50=3.38μM.	19932960
MCF7 MX	Function assay			Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining, IC50=4.07μM.	19932960
BA/F3	Antiproliferative assay			Antiproliferative activity against PDGFRbeta transfected mouse BA/F3 cells, IC50=0.039μM.	20817538
HEK293	Function assay			Inhibition of autophosphorylation of DDR1 expressed in HEK293 cells by ELISA, IC50=0.043μM.	20817538
A31	Function assay			Inhibition of human PDGFRalpha autophosphorylation in human A31 cells by ELISA, IC50=0.072μM.	20817538
A31	Function assay			Inhibition of PDGFRbeta autophosphorylation in human A31 cells by ELISA, IC50=0.072μM.	20817538
GIST882	Function assay			Inhibition of human KIT autophosphorylation in human GIST882 cells by ELISA, IC50=0.097μM.	20817538
GIST882	Antiproliferative assay			Antiproliferative activity against human GIST882 cells, IC50=0.108μM.	20817538
HEK293	Function assay			Inhibition of autophosphorylation of DDR2 expressed in HEK293 cells by ELISA, IC50=0.141μM.	20817538
Ba/F	Function assay			Inhibition of autophosphorylation of BCR-ABL1 expressed in Ba/F cells, IC50=0.221μM.	20817538
K562	Antiproliferative assay			Antiproliferative activity against human K562 cells, IC50=0.244μM.	20817538
HEK293	Function assay			Inhibition of autophosphorylation of CSF1R expressed in HEK293 cells by ELISA, IC50=0.291μM.	20817538
M-NFS-60	Antiproliferative assay			Antiproliferative activity against mouse M-NFS-60 cells, IC50=0.358μM.	20817538
K562	Function assay			Inhibition of BCR-ABL1 autophosphorylation in human K562 cells, IC50=0.473μM.	20817538
BA/F3	Antiproliferative assay			Antiproliferative activity against BCR-ABL1 transfected mouse BA/F3 cells, IC50=0.678μM.	20817538
BA/F3	Antiproliferative assay			Antiproliferative activity mouse BA/F3 cells in presence of interleukin 3, IC50=9.459μM.	20817538
K562	Antiproliferative assay			Antiproliferative activity against human imatinib-resistant K562 cells, IC50=0.00605μM.	21376587
KU812	Antiproliferative assay			Antiproliferative activity against human KU812 cells, IC50=0.337μM.	21376587
K562	Antiproliferative assay			Antiproliferative activity against human K562 cells, IC50=0.38μM.	21376587
Sf9	Function assay			Binding affinity to human active site of N-terminal hexahistidine-tagged ABL2 expressed in Trichoplusia ni infected Sf9 cells by isothermal titration calorimetric assay, Kd=0.006μM.	21417343
Sf9	Function assay			Binding affinity to human remote site of N-terminal hexahistidine-tagged ABL2 expressed in Trichoplusia ni infected Sf9 cells by isothermal titration calorimetric assay, Kd=0.5μM.	21417343
TF1	Cytotoxicity assay			Cytotoxicity against human TF1 cells expressing c-KIT mutation assessed as cell viability, IC50=0.013μM.	22221201
K562	Antiproliferative assay			Antiproliferative activity against human K562 cells, GI50=0.17μM.	22439674
HUVEC	Antiproliferative assay			Antiproliferative activity against HUVEC cells, GI50=18.5μM.	22439674
K562	Antiproliferative assay			Antiproliferative activity against human K562 cells, IC50=0.5μM.	23352483
K562	Cytotoxicity assay			Cytotoxicity against human K562 cells, IC50=0.17μM.	23600806
GIST882	Function assay			Inhibition of KIT K642E mutant autophosphorylation (unknown origin) expressed in human GIST882 cells by ELISA, IC50=0.097μM.	23611771
GIST882	Function assay			Inhibition of KIT K642E mutant (unknown origin) expressed in human GIST882 cells assessed as cell growth inhibition by ATP-depletion assay, IC50=0.108μM.	23611771
32D	Function assay			Inhibition of human BCR-ABL1 (unknown origin) expressed in mouse 32D cells, IC50=0.194μM.	23611771
BA/F3	Function assay			Inhibition of human BCR-ABL1 autophosphorylation expressed in mouse BA/F3 cells by ELISA, IC50=0.221μM.	23611771
BA/F3	Function assay			Inhibition of human BCR-ABL1 expressed in mouse BA/F3 cells assessed as cell growth inhibition by ATP-depletion assay, IC50=0.678μM.	23611771
Sf9	Function assay			Inhibition of recombinant Abl kinase (unknown origin) expressed in Sf9 cells using GGEAIYAAPFKK as substrate in presence of [gamma33P]ATP, IC50=0.3μM.	24681986
HMC-1.2	Antiproliferative assay			Antiproliferative activity against human HMC-1.2 cells carrying V560G, D816V mutant assessed as cell growth inhibition by MTT assay, IC50=17μM.	25004409
K562	Cytotoxicity assay			Cytotoxicity against human K562 cells assessed as reduction in cell viability, IC50=0.06μM.	26264503
IR-K562	Cytotoxicity assay			Cytotoxicity against imatinib resistant human IR-K562 cells assessed as reduction in cell viability, IC50=1.1μM.	26264503
HEK293	Cytotoxicity assay			Cytotoxicity against HEK293 cells assessed as reduction in cell viability, CC50=8.4μM.	26264503
U937	Cytotoxicity assay			Cytotoxicity against human U937 cells assessed as reduction in cell viability, IC50=19μM.	26264503
THP1	Cytotoxicity assay			Cytotoxicity against human THP1 cells assessed as reduction in cell viability, IC50=25μM.	26264503
HCT116	Anticancer assay			Anticancer activity against human HCT116 cells, IC50=34.4μM.	26312434
293T	Cytotoxicity assay			Cytotoxicity against human 293T cells assessed as growth inhibition, CC50=20.53μM.	26850004
K562	Cytotoxicity assay			Cytotoxicity against human K562 cells, IC50=0.5μM.	27189674
Sf9	Function assay			Binding affinity to recombinant full length human N-terminal GST-tagged Syk-KD (356 to 635 residues) cytoplasmic domain expressed in baculovirus infected Sf9 insect cells using poly EY 4:1 as substrate, Ki=5μM.	29132752
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
GIST882	Antiproliferative assay			Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as reduction in cell viability by MTS assay, GI50=0.195μM.	30968693
GIST882	Antiproliferative assay			Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as reduction in cell viability by methylene blue staining based assay, GI50=0.195μM.	30968693
GIST48	Antiproliferative assay			Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as reduction in cell viability by MTS assay, GI50=0.625μM.	30968693
GIST48	Antiproliferative assay			Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as reduction in cell viability by methylene blue staining based assay, GI50=0.625μM.	30968693
Sf9	Function assay			Inhibition of unactivated recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation, IC50=0.769μM.	30968693
GIST430	Antiproliferative assay			Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as reduction in cell viability by MTS assay, GI50=0.929μM.	30968693
GIST430	Antiproliferative assay			Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as reduction in cell viability by methylene blue staining based assay, GI50=0.929μM.	30968693
Sf9	Function assay			Inhibition of ATP-activated recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation, IC50=5.21μM.	30968693
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生物活性

製品説明

Targets

PDGFR ^[1] (Cell-free assay)	c-Kit ^[2] (M-07e cells)	v-Abl ^[1] (Cell-free assay)
100 nM	100 nM	600 nM

In Vitro
In vitro	In vitro assays for inhibition of a panel of tyrosine and serine/threonine protein kinases show that Imatinib inhibits the v-Abl tyrosine kinase and PDGFR potently with an IC50 of 0.6 and 0.1 μM, respectively. ^[1] Imatinib inhibits the SLF-dependent activation of wild-type c-kit kinase activity with a IC50 for these effects of approximately 0.1 μM, which is similar to the concentration required for inhibition of PDGFR. ^[2] Imatinib exhibits growth-inhibitory activity on the human bronchial carcinoid cell line NCI-H727 and the human pancreatic carcinoid cell line BON-1 with an IC50 of 32.4 and 32.8 μM, respectively. ^[3] A recent study shows that Imatinib has the potential to exert its antileukemia effects in chronic myelogenous leukemia by down-regulating hERG1 K(+) channels, which are highly expressed in leukemia cells and appear of exceptional importance in favoring leukemogenesis. ^[4]
Kinase Assay	PDGF receptor kinase activity
Kinase Assay	PDGF receptor is immunoprecipitated from BALB/c 3T3 cell extracts with rabbit antiserum to the murine PDGF receptor for 2 hours on ice. Protein A-Sepharose beads are used to collect the antigen-antibody complexes. The immunoprecipitates are washed twice with TNET (50 mM Tris, pH 7.5, 140 mM NaCl, 5 mM EDTA, 1% Triton X-100), once with TNE (50 mM Tris, pH 7.5, 140 mM EDTA), and once with kinase buffer (20 mM Tris, pH 7.5,10 mM MgCl₂). After stimulation with PDGF (50 ng/mL) for 10 minutes at 4 °C, different concentrations of drug are added to the reaction mixture. PDGF receptor kinase activity is determined by incubation with 10 μCi [7-³³P]-ATP and l μM ATP for 10 minutes at 4 °C. Immune complexes are separated by SDS-PAGE on 7.5% gels.
細胞実験	細胞株	BON-1 cells and NCI-H727 cells
	濃度	~100 μM
	反応時間	48 hours
	実験の流れ	BON-1 cells and NCI-H727 cells are seeded into flat-bottomed 96-well plates in triplicate and allowed to adhere overnight in 10% fetal bovine serum-supplemented DMEM or RPMI 1640 complete medium, respectively; the medium is then exchanged for serum-free medium (negative control) or serum-free medium containing serial dilutions of Imatinib. After 48 hours (control cultures do not reach confluence), the number of metabolically active cells is determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, and absorbance is measured in a Packard Spectra microplate reader at 540 nm. Growth inhibition is calculated using the following formula: inhibition rate = (1 − a / b) × 100%, where a and b are the absorbance values of the treated and control groups, respectively.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	p-STAT3 / STAT3 / p-STAT5 / STAT5 p-ZAP70 / ZAP70 / p-LAT / LAT p-STAT3 / STAT3 / p-STAT5 / STAT5 p-ZAP70 / ZAP70 / p-LAT / LAT		18981115
	Immunofluorescence	RelB Cortactin / F-actin RelB Cortactin / F-actin		20371728
	Growth inhibition assay	Cell viability		28435223

In Vivo
In Vivo	Imatinib produces a different antitumor effect on three xenografted tumors derived from surgical samples of fresh human small cell lung cancers, with 80%, 40% and 78% growth inhibition of SCLC6, SCLC61 and SCLC108 tumors, respectively, and no significant inhibition of SCLC74 growth. ^[5] In high fat fed ApoE(-/-) mice, Imatinib significantly reduces the high fat-induced lipid staining area by 30%, 27% and 35% compared to high-fat diet untreated controls when dosed by gavage at 10, 20 and 40 mg/kg, respectively, and suppresses carotid artery lipid accumulation. ^[6]

In Vivo

Imatinib produces a different antitumor effect on three xenografted tumors derived from surgical samples of fresh human small cell lung cancers, with 80%, 40% and 78% growth inhibition of SCLC6, SCLC61 and SCLC108 tumors, respectively, and no significant inhibition of SCLC74 growth. ^[5]

In high fat fed ApoE(-/-) mice, Imatinib significantly reduces the high fat-induced lipid staining area by 30%, 27% and 35% compared to high-fat diet untreated controls when dosed by gavage at 10, 20 and 40 mg/kg, respectively, and suppresses carotid artery lipid accumulation. ^[6]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05493215	Recruiting	Gastrointestinal Stromal Tumors	Reema A. Patel\|University of Kentucky	March 26 2024	Phase 2
NCT06090669	Recruiting	Inherited Bone Marrow Failure Syndrome\|Familial Platelet Disorder With Predisposition to Myeloid Malignancies	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	December 19 2023	Phase 1
NCT05413915	Recruiting	Chronic Myeloid Leukemia\|Chronic Myeloid Leukemia BCR/ABL-Positive\|Chronic Myeloid Leukemia in Remission	Sarit Assouline\|Novartis\|Sir Mortimer B. Davis - Jewish General Hospital	June 19 2023	Phase 3
NCT05816785	Recruiting	Head and Neck Cancer\|Squamous Cell Carcinoma of Head and Neck	University of Wisconsin Madison\|National Cancer Institute (NCI)	April 18 2023	Early Phase 1
NCT05623774	Recruiting	CML	Inhibikase Therapeutics Inc.	December 16 2022	Phase 1
NCT05282108	Recruiting	Chronic Myeloid Leukemia	Hikma Pharmaceuticals LLC	July 20 2022	--

参考
[1] Buchdunger E, et al. Proc Natl Acad Sci USA. 1995, 92(7), 2558–2562. [2] Heinrich MC, et al. Blood. 2000, 96(3), 925-932. [3] Yao JC, et al. Clin Cancer Res. 2007, 13(1), 234-240. [4] Zheng F, et al. Med Oncol, 2012, 29(3), 2127-2135. [5] Decaudin D, et al. Int J Cancer. 2005, 113(5), 849-856. [6] Ballinger ML, et al. J Cell Mol Med. 2010,14(6B), 1408-1418. + 展開

参考

+ 展開

化学情報

分子量	493.6	化学式	C₂₉H₃₁N₇O
CAS No.	152459-95-5	SDF	Download Imatinib SDFをダウンロードする
Smiles	CC1=C(C=C(C=C1)NC(=O)C2=CC=C(C=C2)CN3CCN(CC3)C)NC4=NC=CC(=N4)C5=CN=CC=C5
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 25 mg/mL ( (50.64 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

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よくある質問（FAQ）

質問1:
Could you please advise whether it is a clear solution for compound dissolved in vehicle 2% DMSO+30% PEG 300+2% Tween 80+ddH2O?

回答
For S2475 Imatinib (STI571), it is soluble in 2% DMSO+30% PEG 300+2% Tween 80+ddH2O at 2mg/ml. When making the solution, please dissolve the compound in DMSO clearly first. If it dissolves not readily, please sonicate and warm it in water bath at 45-50C. Then add PEG and Tween. After they mixed well, dilute with water.

質問2:
What is the difference between S2475 (Imatinib) and S1026 (Imatinib Mesylate)? Are they water soluble?

回答
S2475 is free base of Imatinib while S1026 is a solt form of Imatinib. They have exactly the same biological activity but different solubility. S1026 can be dissolved in water, but S2475 is not soluble in water. S2475 can be dissolved in DMSO at up to 3mg/ml.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):