ホームページ Protein Tyrosine Kinase Bcr-Abl inhibitor - c-Kit inhibitor - PDGFR inhibitor - Autophagy activator Imatinib Mesylate For research use only.

Imatinib Mesylate

別名：CGP-57148B,STI571

Imatinib Mesylate is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib Mesylate (STI571) induces autophagy.

Imatinib Mesylate化学構造

CAS No. 220127-57-1

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 28600 国内在庫あり
JPY 22000 国内在庫あり
JPY 41500 国内在庫あり
JPY 103500 国内在庫あり
JPY 253500 国内在庫なし(納期7~10日)

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（240）

製品安全説明書

現在のバッチを見る： 純度： 99.99%
99.99

Imatinib Mesylate関連製品

シグナル伝達経路

Bcr-Abl Signaling Pathways

Bcr-Ablシグナル伝達経路

Bcr-Abl阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
MCF-7 Growth Inhibition Assay 10 μM 48 h blocks cell proliferation increase induced by BJ3Z 25274034
PC3  Apoptosis Assay 20 μM 48/72 h increases cell survival 25786656
PC3  Cell Viability Assay 20 μM 6-72 h increases cell viability 25786656
DU145 Apoptosis Assay 20 μM 48/72 h induces cell death by apoptosis 25786656
DU145 Cell Viability Assay 20 μM 6-72 h decreases cell viability 25786656
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 = 0.055 μM. 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 = 0.088 μM. 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 = 0.393 μM. 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 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 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 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
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 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 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
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 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
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
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
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
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
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 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 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 S6 phosphorylation at S235/236 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 S6 phosphorylation at S235/236 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting 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
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
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 S6K phosphorylation at T389 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting 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 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
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 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
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 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
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
MDA-MB-23 Cytotoxicity Assay 24 h IC50=1.8 μM 22000207
MCF-7 Cytotoxicity Assay 24 h IC50=0.83 μM 22000207
K562 Cytotoxicity Assay 24 h IC50=0.21 μM 22000207
GIST882 Growth Inhibition Assay 96 h IC50=1.7 μM 24900212
EOL-1 Cytotoxicity assay 72 hrs Cytotoxicity against human EOL-1 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 0.0002 μM. 19301902
EOL-1 Antiproliferative assay 72 hrs Antiproliferative activity against human EOL-1 cells after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.001 μM. 29544149
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 = 0.003 μM. 28541695
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 = 0.008 μM. 27077705
GISTT1 Antiproliferative assay 72 hrs Antiproliferative activity against human GISTT1 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 0.008 μM. 27966954
GISTT1 Function assay 72 hrs Inhibition of KIT in human GISTT1 cells assessed as growth inhibition after 72 hrs by SRB assay, GI50 = 0.01 μM. 23773153
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 = 0.0107 μM. 28541695
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 = 0.014 μM. 27077705
GIST882 Antiproliferative assay 72 hrs Antiproliferative activity against human GIST882 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 0.014 μM. 27966954
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 = 0.017 μM. 30204441
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 = 0.019 μM. 29544149
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 = 0.019 μM. 27966954
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 = 0.02 μM. 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 = 0.0249 μM. 28541695
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 = 0.027 μM. 16415863
HL60 Antiproliferative assay 72 hrs Antiproliferative activity against human HL60 cells assessed as inhibition of cell survival after 72 hrs by MTT assay, IC50 = 0.03 μM. 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 = 0.034 μM. 27010810
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 = 0.034 μM. 29544149
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 = 0.034 μM. 27966954
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 = 0.036 μM. 28541695
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 = 0.039 μM. 27077705
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 = 0.039 μM. 27966954
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 = 0.04 μM. 23241029
GISTT1 Cytotoxicity assay 72 hrs Cytotoxicity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 0.04 μM. 28991465
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 = 0.043 μM. 28280261
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 = 0.045 μM. 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 = 0.0451 μM. 28541695
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 = 0.046 μM. 30204441
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 0.049 μM. 19301902
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 = 0.05 μM. 23241029
HT-29 Antiproliferative assay 96 hrs Antiproliferative activity against human HT-29 cells after 96 hrs by SRB assay, IC50 = 0.06 μM. 19469547
HT-29 Antiproliferative assay 96 hrs Antiproliferative activity against human HT-29 cells after 96 hrs by SRB assay, IC50 = 0.06 μM. 29724653
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 = 0.06 μM. 27011159
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 = 0.07 μM. 30204441
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 = 0.074 μM. 27077705
MEG01 Antiproliferative assay 72 hrs Antiproliferative activity against human MEG01 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 0.074 μM. 27966954
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 = 0.0771 μM. 30137981
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 = 0.089 μM. 26562217
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 = 0.09 μM. 28280261
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 = 0.0905 μM. 30137981
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 = 0.092 μM. 23600806
insect Function assay 30 mins Inhibition of human recombinant wild type ABL1 expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0982 μM. 23301703
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 0.1 μM. 19301902
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 = 0.1 μM. 22221201
BV173 Antiproliferative assay 48 hrs Antiproliferative activity against human BV173 cells after 48 hrs by Cell-Titer-Glo luminescent cell viability assay, GI50 = 0.1 μM. 27011159
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 = 0.1 μM. 27077705
K562 Cytotoxicity assay 24 hrs Cytotoxicity against human K562 cells after 24 hrs by MTT assay, IC50 = 0.1 μM. 22632935
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 = 0.102 μM. 30204441
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 = 0.102 μM. 27966954
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 = 0.11 μM. 28541695
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 = 0.11 μM. 23088644
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 = 0.11 μM. 27966954
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 = 0.112 μM. 16415863
insect cells Function assay 30 mins Inhibition of human recombinant ABL1 M351T mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.1143 μM. 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 = 0.115 μM. 23301703
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 = 0.12 μM. 27077705
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 = 0.129 μM. 23088644
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 = 0.14 μM. 26789553
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 = 0.147 μM. 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 = 0.1482 μM. 28541695
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 = 0.149 μM. 30137981
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 = 0.16 μM. 26789553
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 = 0.16 μM. 27077705
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 = 0.162 μM. 27502700
KU812 Antiproliferative assay 72 hrs Antiproliferative activity against human KU812 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 0.163 μM. 27966954
insect cells Function assay 30 mins Inhibition of human recombinant ABL1 H396P mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.1739 μM. 23301703
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 = 0.19 μM. 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 = 0.19 μM. 16415863
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 = 0.192 μM. 30204441
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by Cell-Titer-Glo luminescent cell viability assay, GI50 = 0.2 μM. 27011159
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 = 0.201 μM. 30137981
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 = 0.216 μM. 30204441
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by trypan blue dye exclusion assay, IC50 = 0.22 μM. 26629859
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 = 0.223 μM. 30204441
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 = 0.223 μM. 27966954
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 = 0.23 μM. 29544149
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 = 0.24 μM. 26789553
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 = 0.24 μM. 23301703
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 = 0.249 μM. 30137981
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 = 0.25 μM. 28280261
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 = 0.257 μM. 16415863
EM2 Antiproliferative assay 48 hrs Antiproliferative activity against human EM2 cells after 48 hrs by Cell-Titer-Glo luminescent cell viability assay, GI50 = 0.26 μM. 27011159
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 0.267 μM. 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 = 0.27 μM. 27966954
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 = 0.272 μM. 28280261
KBM5 Cytotoxicity assay 72 hrs Cytotoxicity against human KBM5 cells harboring wild type Bcr-Abl after 72 hrs by MTT assay, IC50 = 0.28 μM. 20149665
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay, IC50 = 0.28 μM. 26195136
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells assessed as decrease in cell proliferation after 72 hrs by XTT assay, IC50 = 0.31 μM. 27214512
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 = 0.312 μM. 30204441
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 = 0.339 μM. 16415863
HEK293 Function assay 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 = 0.35 μM. 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 = 0.35 μM. 23241029
insect cells Function assay 30 mins Inhibition of human recombinant ABL1 G250E mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.3599 μM. 23301703
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 = 0.362 μM. 23088644
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 = 0.37 μM. 29544149
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells assessed as inhibition of cell survival after 72 hrs by MTT assay, IC50 = 0.38 μM. 26850004
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 = 0.38 μM. 26789553
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 = 0.3819 μM. 28541695
K562 Cytotoxicity assay 48 to 72 hrs Cytotoxicity against human BCR-ABL positive K562 cells after 48 to 72 hrs by MTT assay, IC50 = 0.3844 μM. 22789429
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells after 72 hrs by MTS assay, GI50 = 0.39 μM. 22932313
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 = 0.392 μM. 30204441
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 = 0.4 μM. 27077705
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 = 0.424 μM. 23088644
KCL22 Antiproliferative assay 48 hrs Antiproliferative activity against human KCL22 cells after 48 hrs by Cell-Titer-Glo luminescent cell viability assay, GI50 = 0.43 μM. 27011159
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 = 0.455 μM. 30137981
K562 Cytotoxicity assay 48 hrs Cytotoxicity against human K562 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 0.47 μM. 23735826
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50 = 0.47 μM. 25778766
insect cells Function assay 30 mins Inhibition of human recombinant ABL1 E255K mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.4858 μM. 23301703
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 = 0.5 μM. 22221201
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 = 0.5 μM. 26789553
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells after 72 hrs by calcein-AM assay, IC50 = 0.5 μM. 23981532
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells after 72 hrs using Calcein AM by fluorescence assay, IC50 = 0.5 μM. 25757603
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 = 0.5 μM. 23301703
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50 = 0.5 μM. 23932071
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay, IC50 = 0.51 μM. 26814890
K562 Cytotoxicity assay 48 hrs Cytotoxicity against human K562 cells after 48 hrs by MTT assay, IC50 = 0.53 μM. 26707846
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50 = 0.53 μM. 28525838
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 = 0.535 μM. 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 = 0.567 μM. 30204441
K562 Cytotoxicity assay 48 hrs Cytotoxicity against human K562 cells after 48 hrs by MTT assay, IC50 = 0.58 μM. 21295380
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 = 0.59 μM. 23301703
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 = 0.625 μM. 26789553
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 = 0.625 μM. 27966954
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 = 0.659 μM. 26789553
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 = 0.669 μM. 30204441
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 = 0.68 μM. 26629859
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 = 0.701 μM. 30204441
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by fluorescence microplate reader method, IC50 = 0.73 μM. 26741853
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 = 0.73 μM. 28974338
insect cells Function assay 30 mins Inhibition of human recombinant ABL1 Y253F mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.7496 μM. 23301703
K562 Function assay 2 hrs Inhibition of BCR/ABL p210 autophosphorylation in human K562 cells after 2 hrs by Western blot analysis, IC50 = 0.75 μM. 20188579
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 = 0.803 μM. 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 = 0.8031 μM. 28541695
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 = 0.836 μM. 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 = 0.838 μM. 30137981
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 = 0.85 μM. 27966954
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 = 0.855 μM. 26789553
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 = 0.874 μM. 30137981
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 = 0.96 μM. 23088644
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 = 0.962 μM. 16415863
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 = 1 μM. 30261468
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 = 1 μM. 23301703
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 = 1.1 μM. 28991465
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 = 1.1 μM. 29655981
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50 = 1.16 μM. 26231079
K562 Cytotoxicity assay 48 hrs Cytotoxicity against human K562 cells expressing Bcr-Abl assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 1.16 μM. 26451772
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 = 1.191 μM. 30204441
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 = 1.245 μM. 28541695
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 = 1.274 μM. 20156689
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 = 1.29 μM. 27077705
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 = 1.29 μM. 27966954
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 = 1.444 μM. 23088644
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 = 1.466 μM. 28541695
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 = 1.523 μM. 30204441
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 = 1.6 μM. 23301703
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 = 1.69 μM. 26789553
GIST882 Antiproliferative assay 96 hrs Antiproliferative activity against human GIST882 cells after 96 hrs by SRB assay, IC50 = 1.7 μM. 19469547
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 = 1.7 μM. 29724653
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 = 1.79 μM. 27966954
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 = 1.834 μM. 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 = 1.863 μM. 23088644
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 = 1.93 μM. 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 = 2.1 μM. 26789553
NCI-H1703 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1703 cells after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 2.1 μM. 29544149
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 = 2.16 μM. 27966954
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 = 2.169 μM. 26789553
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 = 2.377 μM. 23088644
HGC27 Antiproliferative assay 96 hrs Antiproliferative activity against human HGC27 cells after 96 hrs by SRB assay, IC50 = 2.4 μM. 19469547
HGC27 Antiproliferative assay 96 hrs Antiproliferative activity against human HGC27 cells after 96 hrs by SRB assay, IC50 = 2.4 μM. 29724653
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 = 2.49 μM. 27077705
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 = 2.49 μM. 27966954
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 = 2.547 μM. 23088644
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 = 2.749 μM. 30204441
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 = 2.9 μM. 23241029
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 = 2.951 μM. 23088644
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 = 3 μM. 26789553
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 = 3 μM. 27077705
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 = 3 μM. 27966954
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 = 3.005 μM. 23088644
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 = 3.3 μM. 23301703
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells after 72 hrs by MTT assay, IC50 = 3.43 μM. 29684708
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 = 3.6 μM. 23301703
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 = 3.763 μM. 23088644
HGC27 Cytotoxicity assay 48 hrs Cytotoxicity against HGC27 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 3.8 μM. 24900584
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 = 3.947 μM. 30204441
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 = 4.1 μM. 26789553
K562 Antiproliferative assay 48 hrs Antiproliferative activity against Bcr/Abl positive human K562 cells after 48 hrs by MTT method, IC50 = 4.12 μM. 25464886
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50 = 4.12 μM. 26298495
HEK293 Function assay 3 mins Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay, IC50 = 4.2 μM. 23241029
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 4.56 μM. 28525838
K562/G Cytotoxicity assay 72 hrs Cytotoxicity against human K562/G cells assessed as cell viability after 72 hrs by MTT assay, IC50 = 4.65 μM. 26814890
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 = 4.686 μM. 28541695
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 = 4.79 μM. 23600806
insect cells Function assay 30 mins Inhibition of human recombinant ABL1 T315I mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 5.155 μM. 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 = 5.2 μM. 23301703
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 = 5.3 μM. 26789553
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50 = 5.4 μM. 21576023
KBM5 Cytotoxicity assay 72 hrs Cytotoxicity against human KBM5 cells harboring Bcr-Abl T315I mutant after 72 hrs by MTT assay, IC50 = 5.4 μM. 20149665
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 = 5.6 μM. 23301703
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 = 6.67 μM. 27077705
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 = 6.67 μM. 27966954
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 = 6.7 μM. 26789553
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 = 6.986 μM. 28541695
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 7.12 μM. 29684708
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 = 7.7 μM. 26789553
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 = 8.437 μM. 20156689
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 = 8.615 μM. 23088644
A2780 Antiproliferative assay 72 hrs Antiproliferative activity against human A2780 cells after 72 hrs by MTT assay, IC50 = 8.9 μM. 29684708
BESM Antitrypanosomal assay 88 hrs Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BESM cells measured after 88 hrs postinfection by HTS assay, EC50 = 9 μM. 20547819
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 = 9.2 μM. 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 = 9.5 μM. 23301703
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 = 9.645 μM. 30137981
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 = 9.7 μM. 26789553
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 = 9.93 μM. 30204441
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 10 μM. 19301902
HepG2 Antiproliferative assay 24 to 96 hrs Antiproliferative activity against human HepG2 cells after 24 to 96 hrs by MTS assay, IC50 = 10 μM. 23932071
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 = 11.1 μM. 23301703
MCF7 Antiproliferative assay 96 hrs Antiproliferative activity against human MCF7 cells after 96 hrs by SRB assay, IC50 = 11.3 μM. 29724653
MCF7 Antiproliferative assay 96 hrs Antiproliferative activity against human MCF7 cells after 96 hrs by SRB assay, IC50 = 11.5 μM. 19469547
RKOp21 Cytotoxicity assay 72 hrs Cytotoxicity against human RKOp21 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 12 μM. 19301902
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 = 12.2 μM. 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 = 12.2 μM. 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 = 12.5 μM. 23301703
RKOp21 Cytotoxicity assay 72 hrs Cytotoxicity against human RKOp21 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 12.5892 μM. 19301902
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 = 13 μM. 24681986
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 13.5 μM. 23301703
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 = 14.5 μM. 26562217
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 15.5 μM. 19301902
K562 Antiproliferative assay 48 hrs Antiproliferative activity against imatinib-resistant human K562 cells after 48 hrs by MTT assay, IC50 = 15.7 μM. 26231079
MDA-MB-468 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA-MB-468 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 15.8489 μM. 19301902
KG1a Antiproliferative assay 72 hrs Antiproliferative activity against human KG1a cells assessed as inhibition of cell survival after 72 hrs by MTT assay, IC50 = 16.7 μM. 26850004
MDA-MB-468 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA-MB-468 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 17 μM. 19301902
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 = 17.083 μM. 23088644
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CCK-8 assay, IC50 = 18.52 μM. 23088644
HeLa Cytotoxicity assay 72 hrs Cytotoxicity against human HeLa cells after 72 hrs by alamar-blue cell viability assay, IC50 = 18.65 μM. 19301902
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 = 18.7 μM. 19469547
Hec1A Cytotoxicity assay 72 hrs Cytotoxicity against human Hec1A cells after 72 hrs by alamar-blue cell viability assay, IC50 = 19 μM. 19301902
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 19.66 μM. 29684708
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 = 19.8 μM. 29724653
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 19.9526 μM. 19301902
CAL27 Cytotoxicity assay 72 hrs Cytotoxicity against human CAL27 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 19.9526 μM. 19301902
Hec1A Cytotoxicity assay 72 hrs Cytotoxicity against human Hec1A cells after 72 hrs by alamar-blue cell viability assay, IC50 = 19.9526 μM. 19301902
GIST48B Growth inhibition assay 72 hrs Growth inhibition of human GIST48B cells after 72 hrs by SRB assay, GI50 = 20 μM. 23773153
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 = 20 μM. 24681986
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 = 20.03 μM. 28974338
CAL27 Cytotoxicity assay 72 hrs Cytotoxicity against human CAL27 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 22 μM. 19301902
H460 Cytotoxicity assay 72 hrs Cytotoxicity against human H460 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 24 μM. 19301902
PC3 Cytotoxicity assay 72 hrs Cytotoxicity against human PC3 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 24 μM. 19301902
HCT15 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT15 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 25 μM. 19301902
HeLa Cytotoxicity assay 72 hrs Cytotoxicity against human HeLa cells after 72 hrs by alamar-blue cell viability assay, IC50 = 25.1189 μM. 19301902
H460 Cytotoxicity assay 72 hrs Cytotoxicity against human H460 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 25.1189 μM. 19301902
HCT15 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT15 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 25.1189 μM. 19301902
PC3 Cytotoxicity assay 72 hrs Cytotoxicity against human PC3 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 25.1189 μM. 19301902
Saos2 Cytotoxicity assay 72 hrs Cytotoxicity against human Saos2 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 25.1189 μM. 19301902
HEK293 Function assay 3 mins Inhibition of human OCT3-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay, IC50 = 25.5 μM. 23241029
Saos2 Cytotoxicity assay 72 hrs Cytotoxicity against human Saos2 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 26 μM. 19301902
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 30 μM. 19301902
A431 Cytotoxicity assay 72 hrs Cytotoxicity against human A431 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 31 μM. 19301902
H69 Cytotoxicity assay 72 hrs Cytotoxicity against human H69 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 31.6228 μM. 19301902
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 31.6228 μM. 19301902
A431 Cytotoxicity assay 72 hrs Cytotoxicity against human A431 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 31.6228 μM. 19301902
H69 Cytotoxicity assay 72 hrs Cytotoxicity against human H69 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 32 μM. 19301902
BESM Cytotoxicity assay 88 hrs Cytotoxicity against BESM cells after 88 hrs by HTS assay, EC50 = 32 μM. 20547819
CCRF-CEM Cytotoxicity assay 72 hrs Cytotoxicity against human CCRF-CEM cells after 72 hrs by alamar-blue cell viability assay, IC50 = 36 μM. 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 = 37 μM. 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 = 37 μM. 19301902
WM266.4 Cytotoxicity assay 72 hrs Cytotoxicity against human WM266.4 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 37 μM. 19301902
U87MG Cytotoxicity assay 72 hrs Cytotoxicity against human U87MG cells after 72 hrs by alamar-blue cell viability assay, IC50 = 38 μM. 19301902
SKBR3 Cytotoxicity assay 72 hrs Cytotoxicity against human SKBR3 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 39 μM. 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 = 39.8107 μM. 19301902
SKBR3 Cytotoxicity assay 72 hrs Cytotoxicity against human SKBR3 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 39.8107 μM. 19301902
AsPC1 Cytotoxicity assay 72 hrs Cytotoxicity against human AsPC1 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 39.8107 μM. 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 = 39.8107 μM. 19301902
CCRF-CEM Cytotoxicity assay 72 hrs Cytotoxicity against human CCRF-CEM cells after 72 hrs by alamar-blue cell viability assay, IC50 = 39.8107 μM. 19301902
U87MG Cytotoxicity assay 72 hrs Cytotoxicity against human U87MG cells after 72 hrs by alamar-blue cell viability assay, IC50 = 39.8107 μM. 19301902
WM266.4 Cytotoxicity assay 72 hrs Cytotoxicity against human WM266.4 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 39.8107 μM. 19301902
AsPC1 Cytotoxicity assay 72 hrs Cytotoxicity against human AsPC1 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 44 μM. 19301902
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 = 45 μM. 24681986
A2780 Cytotoxicity assay 72 hrs Cytotoxicity against human A2780 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 48 μM. 19301902
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
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) 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) phosphorylation transfected in mouse Ba/F3 cells after 1 hr by Western blot analysis 23600806
K562 Function assay 6 hrs Inhibition of BCR-ABL-mediated STAT5 phosphorylation in human K562 cells after 6 hrs by phospho-flow cytometry 22148584
K-562  Growth Inhibition Assay IC50=1 μM 25239662
K562 Growth Inhibition Assay EC50=0.09 μM 16678414
K562r Growth Inhibition Assay IC50=10 μM 24939418
K562  Growth Inhibition Assay IC50=0.5 μM 24939418
Hep G2 Growth Inhibition Assay IC50=31 μM 25863232
T47D  Growth Inhibition Assay IC50=50 μM 25863232
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 = 0.006 μM. 21417343
K562 Antiproliferative assay Antiproliferative activity against human imatinib-resistant K562 cells, IC50 = 0.00605 μM. 21376587
TF1 Cytotoxicity assay Cytotoxicity against human TF1 cells expressing c-KIT mutation assessed as cell viability, IC50 = 0.013 μM. 22221201
BA/F3 Antiproliferative assay Antiproliferative activity against PDGFRbeta transfected mouse BA/F3 cells, IC50 = 0.039 μM. 20817538
HEK293 Function assay Inhibition of autophosphorylation of DDR1 expressed in HEK293 cells by ELISA, IC50 = 0.043 μM. 20817538
MO7e Function assay Inhibition of SCF-induced phosphorylation of c-Kit in MO7e cells by TR-FRET assay, IC50 = 0.046 μM. 18447379
K562 Cytotoxicity assay Cytotoxicity against human K562 cells assessed as reduction in cell viability, IC50 = 0.06 μM. 26264503
A31 Function assay Inhibition of PDGFRbeta autophosphorylation in human A31 cells by ELISA, IC50 = 0.072 μM. 20817538
A31 Function assay Inhibition of human PDGFRalpha autophosphorylation in human A31 cells by ELISA, IC50 = 0.072 μM. 20817538
GIST882 Function assay Inhibition of human KIT autophosphorylation in human GIST882 cells by ELISA, IC50 = 0.097 μM. 20817538
GIST882 Function assay Inhibition of KIT K642E mutant autophosphorylation (unknown origin) expressed in human GIST882 cells by ELISA, IC50 = 0.097 μM. 23611771
GIST882 Antiproliferative assay Antiproliferative activity against human GIST882 cells, IC50 = 0.108 μM. 20817538
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 = 0.108 μM. 23611771
K562 Cytotoxicity assay Cytotoxic effect in K562 cells, IC50 = 0.11 μM. 12951113
HEK293 Function assay Inhibition of autophosphorylation of DDR2 expressed in HEK293 cells by ELISA, IC50 = 0.141 μM. 20817538
K562 Cytotoxicity assay Cytotoxicity against human K562 cells, IC50 = 0.17 μM. 23600806
K562 Antiproliferative assay Antiproliferative activity against human K562 cells, GI50 = 0.17 μM. 22439674
K562 Cytotoxicity assay Cytotoxicity against K562 cells by MTT assay, IC50 = 0.18 μM. 17572088
K562 Antiproliferative assay Antiproliferative activity against K562 cells, IC50 = 0.182 μM. 16332440
32D Cytotoxicity assay Cytotoxic activity against mouse 32D cells transfected with p210 Bcr-abl, IC50 = 0.19 μM. 16415863
32D Function assay Inhibition of human BCR-ABL1 (unknown origin) expressed in mouse 32D cells, IC50 = 0.194 μM. 23611771
Sf9 Function assay Inhibition of human Lyn kinase expressed in Sf9 cells, IC50 = 0.22 μM. 17376680
Ba/F Function assay Inhibition of autophosphorylation of BCR-ABL1 expressed in Ba/F cells, IC50 = 0.221 μM. 20817538
BA/F3 Function assay Inhibition of human BCR-ABL1 autophosphorylation expressed in mouse BA/F3 cells by ELISA, IC50 = 0.221 μM. 23611771
CHO Function assay Inhibition of wild type Platelet-derived growth factor receptor beta phosphorylation in CHO cells, IC50 = 0.24 μM. 12166950
K562 Antiproliferative assay Antiproliferative activity against human K562 cells, IC50 = 0.244 μM. 20817538
CHO Function assay Inhibition of chimeric PDGF receptor with c-kit cytoplasmic domain phosphorylation in CHO cells, IC50 = 0.26 μM. 12166950
HEK293 Function assay Inhibition of autophosphorylation of CSF1R expressed in HEK293 cells by ELISA, IC50 = 0.291 μM. 20817538
Sf9 Function assay Inhibition of recombinant Abl kinase (unknown origin) expressed in Sf9 cells using GGEAIYAAPFKK as substrate in presence of [gamma33P]ATP, IC50 = 0.3 μM. 24681986
ALL3 Cytotoxicity assay Cytotoxicity against Philadelphia chromosome positive human ALL3 cells by Alamar Blue fluorescent assay, IC50 = 0.333 μM. 19889540
KU812 Antiproliferative assay Antiproliferative activity against human KU812 cells, IC50 = 0.337 μM. 21376587
CML Antiproliferative assay Antiproliferative activity against human CML cells, IC50 = 0.35 μM. 19219016
M-NFS-60 Antiproliferative assay Antiproliferative activity against mouse M-NFS-60 cells, IC50 = 0.358 μM. 20817538
BAF3 Function assay 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 = 0.37 μM. 27966954
K562 Antiproliferative assay Antiproliferative activity against human K562 cells, IC50 = 0.38 μM. 21376587
K562 Function assay Inhibitory activity against human K562 cells growth using MTT assay, IC50 = 0.4 μM. 14552760
Sf9 Function assay Inhibition of human Abl kinase expressed in Sf9 cells, IC50 = 0.47 μM. 17376680
K562 Function assay Inhibition of BCR-ABL1 autophosphorylation in human K562 cells, IC50 = 0.473 μM. 20817538
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 = 0.5 μM. 21417343
K562 Antiproliferative assay Antiproliferative activity against human K562 cells, IC50 = 0.5 μM. 23352483
K562 Cytotoxicity assay Cytotoxicity against human K562 cells, IC50 = 0.5 μM. 27189674
Sf9 Function assay TP_TRANSPORTER: inhibition of ATPase activity in BCRP-expressing Sf9 cells, IC50 = 0.5 μM. 15155841
BA/F3 Antiproliferative assay Antiproliferative activity against BCR-ABL1 transfected mouse BA/F3 cells, IC50 = 0.678 μM. 20817538
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 = 0.678 μM. 23611771
Sf9 Function assay TP_TRANSPORTER: efflux of Hoechst33342 in BCRP-expressing Sf9 cells, IC50 = 0.9 μM. 15155841
CHO Function assay Inhibition of chimeric PDGF receptor with CSF-1R cytoplasmic domain phosphorylation in CHO cells, IC50 = 0.96 μM. 12166950
IR-K562 Cytotoxicity assay Cytotoxicity against imatinib resistant human IR-K562 cells assessed as reduction in cell viability, IC50 = 1.1 μM. 26264503
MDCK Function assay Inhibition of BCRP expressed in MDCK cells by pheophorbide A assay, IC50 = 3.38 μM. 19932960
MCF7 MX Function assay Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining, IC50 = 4.07 μM. 19932960
MCF7 Function assay Inhibition of ABCG2 in human mitoxantrone-resistant MCF7 cells by Hoechst 33342 assay, IC50 = 4.89779 μM. 18678495
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 = 5 μM. 29132752
BaF3 Antiproliferative assay Antiproliferative activity against murine BaF3 cells expressing wild type NPM/ALK by [3H]thymidine uptake assay, IC50 = 7.1 μM. 16970400
A2780 Function assay Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay, IC50 = 7.24436 μM. 18678495
A2780/ADR Function assay Inhibition of P-glycoprotein expressed in A2780/ADR cells by calcein AM assay, IC50 = 7.24436 μM. 17890094
HEK293 Cytotoxicity assay Cytotoxicity against HEK293 cells assessed as reduction in cell viability, CC50 = 8.4 μM. 26264503
BaF3 Antiproliferative assay Antiproliferative activity against murine BaF3 cells expressing NPM/ALK L256T mutant by [3H]thymidine uptake assay, IC50 = 9.1 μM. 16970400
BA/F3 Antiproliferative assay Antiproliferative activity mouse BA/F3 cells in presence of interleukin 3, IC50 = 9.459 μM. 20817538
U937 Antiproliferative assay Antiproliferative activity against U937 cells, IC50 = 14 μM. 16332440
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 = 17 μM. 25004409
HUVEC Antiproliferative assay Antiproliferative activity against HUVEC cells, GI50 = 18.5 μM. 22439674
U937 Cytotoxicity assay Cytotoxicity against human U937 cells assessed as reduction in cell viability, IC50 = 19 μM. 26264503
32D Cytotoxicity assay Cytotoxic activity against mouse 32D Bcr-abl negative cells, IC50 = 20 μM. 16415863
293T Cytotoxicity assay Cytotoxicity against human 293T cells assessed as growth inhibition, CC50 = 20.53 μM. 26850004
THP1 Cytotoxicity assay Cytotoxicity against human THP1 cells assessed as reduction in cell viability, IC50 = 25 μM. 26264503
HCT116 Anticancer assay Anticancer activity against human HCT116 cells, IC50 = 34.4 μM. 26312434
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells 29435139
LAMA-84 Growth Inhibition assay Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50 = 0.07304 μM. SANGER
EM-2 Growth Inhibition assay Inhibition of human EM-2 cell growth in a cell viability assay, IC50 = 0.0888 μM. SANGER
MEG-01 Growth Inhibition assay Inhibition of human MEG-01 cell growth in a cell viability assay, IC50 = 0.08921 μM. SANGER
BV-173 Growth Inhibition assay Inhibition of human BV-173 cell growth in a cell viability assay, IC50 = 0.1874 μM. SANGER
K-562 Growth Inhibition assay Inhibition of human K-562 cell growth in a cell viability assay, IC50 = 0.22432 μM. SANGER
CGTH-W-1 Growth Inhibition assay Inhibition of human CGTH-W-1 cell growth in a cell viability assay, IC50 = 0.38374 μM. SANGER
ST486 Growth Inhibition assay Inhibition of human ST486 cell growth in a cell viability assay, IC50 = 0.6854 μM. SANGER
NCI-H1436 Growth Inhibition assay Inhibition of human NCI-H1436 cell growth in a cell viability assay, IC50 = 0.97801 μM. SANGER
NOS-1 Growth Inhibition assay Inhibition of human NOS-1 cell growth in a cell viability assay, IC50 = 1.65383 μM. SANGER
A498 Growth Inhibition assay Inhibition of human A498 cell growth in a cell viability assay, IC50 = 2.57223 μM. SANGER
BE-13 Growth Inhibition assay Inhibition of human BE-13 cell growth in a cell viability assay, IC50 = 2.62106 μM. SANGER
SUP-T1 Growth Inhibition assay Inhibition of human SUP-T1 cell growth in a cell viability assay, IC50 = 3.82907 μM. SANGER
NCI-H1770 Growth Inhibition assay Inhibition of human NCI-H1770 cell growth in a cell viability assay, IC50 = 5.57262 μM. SANGER
IMR-5 Growth Inhibition assay Inhibition of human IMR-5 cell growth in a cell viability assay, IC50 = 6.22147 μM. SANGER
LB2241-RCC Growth Inhibition assay Inhibition of human LB2241-RCC cell growth in a cell viability assay, IC50 = 8.07384 μM. SANGER
TGBC24TKB Growth Inhibition assay Inhibition of human TGBC24TKB cell growth in a cell viability assay, IC50 = 8.34052 μM. SANGER
SCC-15 Growth Inhibition assay Inhibition of human SCC-15 cell growth in a cell viability assay, IC50 = 10.7788 μM. SANGER
BB49-HNC Growth Inhibition assay Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50 = 14.3335 μM. SANGER
ES7 Growth Inhibition assay Inhibition of human ES7 cell growth in a cell viability assay, IC50 = 14.7379 μM. SANGER
LB2518-MEL Growth Inhibition assay Inhibition of human LB2518-MEL cell growth in a cell viability assay, IC50 = 16.6094 μM. SANGER
NCI-H510A Growth Inhibition assay Inhibition of human NCI-H510A cell growth in a cell viability assay, IC50 = 17.2442 μM. SANGER
TE-441-T Growth Inhibition assay Inhibition of human TE-441-T cell growth in a cell viability assay, IC50 = 17.2886 μM. SANGER
HH Growth Inhibition assay Inhibition of human HH cell growth in a cell viability assay, IC50 = 17.3999 μM. SANGER
LC4-1 Growth Inhibition assay Inhibition of human LC4-1 cell growth in a cell viability assay, IC50 = 18.0652 μM. SANGER
KARPAS-45 Growth Inhibition assay Inhibition of human KARPAS-45 cell growth in a cell viability assay, IC50 = 18.1848 μM. SANGER
LB1047-RCC Growth Inhibition assay Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50 = 18.4452 μM. SANGER
NKM-1 Growth Inhibition assay Inhibition of human NKM-1 cell growth in a cell viability assay, IC50 = 19.3552 μM. SANGER
SCLC-21H Growth Inhibition assay Inhibition of human SCLC-21H cell growth in a cell viability assay, IC50 = 20.1246 μM. SANGER
RS4-11 Growth Inhibition assay Inhibition of human RS4-11 cell growth in a cell viability assay, IC50 = 20.3308 μM. SANGER
ALL-PO Growth Inhibition assay Inhibition of human ALL-PO cell growth in a cell viability assay, IC50 = 20.8149 μM. SANGER
GDM-1 Growth Inhibition assay Inhibition of human GDM-1 cell growth in a cell viability assay, IC50 = 22.5945 μM. SANGER
DMS-79 Growth Inhibition assay Inhibition of human DMS-79 cell growth in a cell viability assay, IC50 = 24.4934 μM. SANGER
MPP-89 Growth Inhibition assay Inhibition of human MPP-89 cell growth in a cell viability assay, IC50 = 25.6874 μM. SANGER
NB10 Growth Inhibition assay Inhibition of human NB10 cell growth in a cell viability assay, IC50 = 26.47 μM. SANGER
LS-513 Growth Inhibition assay Inhibition of human LS-513 cell growth in a cell viability assay, IC50 = 26.8847 μM. SANGER
L-540 Growth Inhibition assay Inhibition of human L-540 cell growth in a cell viability assay, IC50 = 26.9143 μM. SANGER
ES1 Growth Inhibition assay Inhibition of human ES1 cell growth in a cell viability assay, IC50 = 27.521 μM. SANGER
NTERA-S-cl-D1 Growth Inhibition assay Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay, IC50 = 30.5093 μM. SANGER
EW-1 Growth Inhibition assay Inhibition of human EW-1 cell growth in a cell viability assay, IC50 = 32.9454 μM. SANGER
Calu-6 Growth Inhibition assay Inhibition of human Calu-6 cell growth in a cell viability assay, IC50 = 33.1855 μM. SANGER
CTV-1 Growth Inhibition assay Inhibition of human CTV-1 cell growth in a cell viability assay, IC50 = 33.9789 μM. SANGER
YT Growth Inhibition assay Inhibition of human YT cell growth in a cell viability assay, IC50 = 38.5209 μM. SANGER
TE-6 Growth Inhibition assay Inhibition of human TE-6 cell growth in a cell viability assay, IC50 = 41.2797 μM. SANGER
HT-144 Growth Inhibition assay Inhibition of human HT-144 cell growth in a cell viability assay, IC50 = 41.5486 μM. SANGER
EW-13 Growth Inhibition assay Inhibition of human EW-13 cell growth in a cell viability assay, IC50 = 42.2791 μM. SANGER
KALS-1 Growth Inhibition assay Inhibition of human KALS-1 cell growth in a cell viability assay, IC50 = 43.1328 μM. SANGER
MOLT-16 Growth Inhibition assay Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50 = 45.0752 μM. SANGER
D-336MG Growth Inhibition assay Inhibition of human D-336MG cell growth in a cell viability assay, IC50 = 45.9599 μM. SANGER
TE-11 Growth Inhibition assay Inhibition of human TE-11 cell growth in a cell viability assay, IC50 = 46.653 μM. SANGER
EB2 Growth Inhibition assay Inhibition of human EB2 cell growth in a cell viability assay, IC50 = 46.699 μM. SANGER
SK-N-DZ Growth Inhibition assay Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50 = 48.0961 μM. SANGER
SW684 Growth Inhibition assay Inhibition of human SW684 cell growth in a cell viability assay, IC50 = 48.2695 μM. SANGER
EW-18 Growth Inhibition assay Inhibition of human EW-18 cell growth in a cell viability assay, IC50 = 48.4395 μM. SANGER
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生物活性

製品説明 Imatinib Mesylate is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib Mesylate (STI571) induces autophagy.
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
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-ZAP70 / ZAP70 / p-LAT / LAT p-STAT3 / STAT3 / p-STAT5 / STAT5 18981115
Immunofluorescence Cortactin / F-actin RelB 20937825
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]
動物実験 動物モデル SCLC6, SCLC61, SCLC 74 and SCLC108 small cell lung cancers are injected into Swiss mice (nu/nu, female).
投与量 70 or 100 mg/kg
投与経路 Administered via i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05623774 Recruiting
CML
Inhibikase Therapeutics Inc.
 December 16 2022 Phase 1
NCT02687425 Unknown status
Leukemia Myelogenous Chronic BCR-ABL Positive
Meng Li|Tongji Hospital
 February 2016 Phase 2
NCT02303899 Completed
Mesothelioma Malignant
Istituto Clinico Humanitas
 November 2014 Phase 2
NCT01898377 Terminated
Chronic Graft-versus-host Disease
Seoul National University Hospital
 August 2013 Phase 2
NCT02891395 Completed
Graft Versus Host Disease
University Hospital Lille|Novartis
 December 24 2012 Phase 2

化学情報

分子量 589.71 化学式

C29H31N7O.CH4SO3
CAS No. 220127-57-1 SDF Download Imatinib Mesylate 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.CS(=O)(=O)O
保管

In vitro
Batch:

DMSO : 118 mg/mL ( (200.09 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 : 118 mg/mL

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

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）

mg/kg g μL 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

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