ABT-737

製品コード：S1002 純度：99.98%

ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. ABT-737 induces mitochondrial pathway apoptosis and mitophagy. Phase 2.

CAS No. 852808-04-9

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫なし(納期7~10日)
5mg	JPY 25000	国内在庫あり
50mg	JPY 85500	国内在庫あり
1g	JPY 445500	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（368）

製品安全説明書

現在のバッチを見る：純度： 99.98%

99.98

ABT-737関連製品

関連ターゲット	Bcl-2 Bcl-B Bcl-w Bcl-xL Mcl-1 Bax Bfl-1 Bad Bcl-xL	もっと見る
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関連化合物ライブラリー	Autophagy Compound Library Apoptosis Compound Library Ferroptosis Compound Library Pyroptosis Compound Library Mitochondria-Targeted Compound Library	もっと見る

シグナル伝達経路

Bcl-2シグナル伝達経路

Bcl-2阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
DMS53	Function assay	5 to 10 uM	12 hrs	Inhibition of BCl-2/Bax interaction in human DMS53 cells harboring p53 mutant at 5 to 10 uM after 12 hrs by immunoprecipitation method	26982372
DMS53	Apoptosis assay	5 to 10 uM	12 hrs	Induction of apoptosis in human DMS53 cells harboring p53 mutant assessed as caspase-3 cleavage at 5 to 10 uM after 12 hrs by immunoblotting method	26982372
DMS53	Apoptosis assay	5 to 10 uM	12 hrs	Induction of apoptosis in human DMS53 cells harboring p53 mutant assessed as PARP cleavage at 5 to 10 uM after 12 hrs by immunoblotting method	26982372
DMS53	Function assay	5 to 10 uM	12 hrs	Inhibition of BCl-2/Bim interaction in human DMS53 cells harboring p53 mutant at 5 to 10 uM after 12 hrs by immunoprecipitation method	26982372
DMS53	Apoptosis assay	5 to 10 uM	12 hrs	Induction of apoptosis in human DMS53 cells harboring p53 mutant assessed as cytochrome c release at 5 to 10 uM after 12 hrs by immunoblotting method	26982372
RS4:11	Apoptosis assay	10 uM	24 hrs	Induction of apoptosis in human RS4:11 cells at 10 uM incubated for 24 hrs by Annexin V and propidium iodide staining based FACS method	23047228
IM9	Apoptosis assay	10 uM	24 hrs	Induction of apoptosis in human IM9 cells at 10 uM incubated for 24 hrs by Annexin V and propidium iodide staining based FACS method	23047228
BP3	Apoptosis assay	10 uM	24 hrs	Induction of apoptosis in human BP3 cells at 10 uM incubated for 24 hrs by Annexin V and propidium iodide staining based FACS method	23047228
MDA-MB-231	Function assay	0.03 to 1 uM	1 hr	Antagonist activity at recombinant Bcl-XL assessed as restoration of BIM BH3-induced cytochrome c release in mitochondria isolated from MDA-MB-231 cells at 0.03 to 1 uM after 1 hr by Western blot analysis	22747598
MDA-MB-231	Function assay	0.03 to 1 uM	1 hr	Antagonist activity at recombinant Bcl-XL assessed as restoration of BIM BH3-induced Smac protein release in mitochondria isolated from MDA-MB-231 cells at 0.03 to 1 uM after 1 hr by Western blot analysis	22747598
HeLa	Function assay	10 uM	16 hrs	Inhibition of Rluc-Bax/eYFP-Bcl-xL interaction expressed in human HeLa cells at 10 uM after 16 hrs by BRET assay	22425031
HeLa	Function assay	1 uM	12 hrs	Induction of Bcl-xL-mediated apoptosis in doxycyclin-stimulated human HeLa cells overexpressing Noxa at 1 uM after 12 hrs by Hoechst staining	22386982
BL21	Function assay	10 uM	3 hrs	Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 Y101H mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.38 μM.	21807512
BL21	Function assay	10 uM	3 hrs	Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 F97V mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.3 μM.	21807512
BL21	Function assay	10 uM	3 hrs	Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 L130G mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.29 μM.	21807512
BL21	Function assay	10 uM	3 hrs	Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 A142T mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.27 μM.	21807512
BL21	Function assay	10 uM	3 hrs	Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 V141A mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.19 μM.	21807512
BL21	Function assay	10 uM	3 hrs	Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 R100E mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.16 μM.	21807512
BL21	Function assay	10 uM	3 hrs	Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 L130A mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.073 μM.	21807512
BL21	Function assay	10 uM	3 hrs	Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 delta136T mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.06 μM.	21807512
BL21	Function assay	10 uM	3 hrs	Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 L130V mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.058 μM.	21807512
BL21	Function assay	10 uM	3 hrs	Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 A142G mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.021 μM.	21807512
BL21	Function assay	10 uM	3 hrs	Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 A142Gdelta136T mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.01 μM.	21807512
BL21	Function assay	10 uM	3 hrs	Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 E96G mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.0058 μM.	21807512
BL21	Function assay	10 uM	3 hrs	Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 E129H mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.0045 μM.	21807512
BL21	Function assay	10 uM	3 hrs	Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Wild type Bcl-2-like protein 1 expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.0034 μM.	21807512
BL21	Function assay	10 uM	3 hrs	Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 Y195F mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.0015 μM.	21807512
BL21	Function assay	10 uM	3 hrs	Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 A93V mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.0014 μM.	21807512
BL21	Function assay	10 uM	3 hrs	Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 G196A mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.001 μM.	21807512
RS4;11	Function Assay	100 nM	1/3/6 h	induces caspase-dependent Mcl-1 cleavage	24951472
OPM-2	Apoptosis Assay	125/250/500 nM	48h	induces cell apoptosis in a dose-dependent manner	25008202
COG-LL-319	Function Assay	100 nM	1/3/6 h	induces caspase-dependent Mcl-1 cleavage	24951472
RPMI-8226	Apoptosis Assay	125/250/500 nM	48h	induces cell apoptosis in a dose-dependent manner	25008202
OPM-2	Cell Viability Assay	125/250/500 nM	48h	decreases cell viability in a dose-dependent manner	25008202
RPMI-8226	Cell Viability Assay	125/250/500 nM	48h	decreases cell viability in a dose-dependent manner	25008202
Caco2	Apoptosis Assay	1/5/10 μM	48 h	causes cell death in a dose-dependent manner	25192188
Colo205	Apoptosis Assay	1/5/10 μM	48 h	causes cell death in a dose-dependent manner	25192188
SW480	Apoptosis Assay	1/5/10 μM	48 h	causes cell death in a dose-dependent manner	25192188
HT29	Apoptosis Assay	1/5/10 μM	48 h	causes cell death in a dose-dependent manner	25192188
CX-1	Growth Inhibition Assay	0.2–60 μM	72 h	IC50=1.8 μM	25208882
LS174T	Growth Inhibition Assay	0.2–60 μM	72 h	IC50=18.3 μM	25208882
Clone A	Growth Inhibition Assay	0.2–60 μM	72 h	IC50=7.5 μM	25208882
MM.1S	Function Assay	500/750 nM	24/48 h	downregulates Bim, principally the EL isoform	25208888
U266	Function Assay	500/750 nM	24/48 h	downregulates Bim, principally the EL isoform	25208888
RPMI8226	Function Assay	500/750 nM	24/48 h	downregulates Bim, principally the EL isoform	25208888
A5-RT3	Function Assay	5 μM	6 h	induces the release of mitochondrial proteins and reduces clonogenic survival in a caspase-independent manner	25210795
HaCaT	Function Assay	10 μM	24/48 h	induces MMP and DNA fragmentation	25210795
A5-RT3	Function Assay	10 μM	24/48 h	induces MMP and DNA fragmentation	25210795
HaCaT	Cell Viability Assay	0.1/1/10 μM	24 h	decreases cell viability in a dose-dependent manner	25210795
A5-RT3	Cell Viability Assay	0.1/1/10 μM	24 h	decreases cell viability in a dose-dependent manner	25210795
HCT116	Cell Viability Assay	0-10 μM	24 h	IC50=20.49 µM	25304383
LS411N	Cell Viability Assay	0-10 μM	24 h	IC50=11.47 µM	25304383
SW620	Cell Viability Assay	0-10 μM	24 h	IC50=12.24 µM	25304383
Caco-2	Cell Viability Assay	0-10 μM	24 h	IC50=19.7 µM	25304383
DLD1	Cell Viability Assay	0-10 μM	24 h	IC50=18.78 µM	25304383
RL	Cell Viability Assay	0.0001-1 μM	96 h	decreases the cell viability in a dose-dependent manner	25373508
RKO	Cell Viability Assay	0-10 μM	24 h	IC50> 25 µM	25304383
OcI-LY18	Cell Viability Assay	0.0001-1 μM	96 h	decreases the cell viability in a dose-dependent manner	25373508
H1299	Apoptosis Assay	20 μM	48 h	induces apoptosis significantly combined with aspirin	25388762
Sc-1	Cell Viability Assay	0.0001-1 μM	96 h	decreases the cell viability in a dose-dependent manner	25373508
A549	Apoptosis Assay	20 μM	48 h	induces apoptosis significantly combined with aspirin	25388762
HT-29	Cell Viability Assay	0-20 μM	72 h	decreases the cell survival in a dose-dependent manner combined with aspirin	25388762
HCT-116	Cell Viability Assay	0-20 μM	72 h	decreases the cell survival in a dose-dependent manner combined with aspirin	25388762
HO-8910	Cell Viability Assay	0-20 μM	72 h	decreases the cell survival in a dose-dependent manner combined with aspirin	25388762
H1299	Cell Viability Assay	0-20 μM	72 h	decreases the cell survival in a dose-dependent manner combined with aspirin	25388762
ZR-75-1	Function Assay	5 μM	24 h	enhances thelevel of Mcl-1 expression	25409124
A549	Cell Viability Assay	0-20 μM	72 h	decreases the cell survival in a dose-dependent manner combined with aspirin	25388762
MCF-7	Function Assay	5 μM	24 h	enhances thelevel of Mcl-1 expression	25409124
MDA-MB 231	Function Assay	5 μM	24 h	enhances thelevel of Mcl-1 expression	25409124
MCF-7	Apoptosis Assay	5 μM	4/24/48 h	increases the cleaved PARP	25409124
MCF-7	Cell Viability Assay	5 μM	48 h	enhances the sensitivity to or radiation	25409124
K562	Cell Viability Assay	1-10 μM	48 h	IC50=26.7 μM	25596561
U87	Function Assay	50 μM	24 h	reduces the mRNA expression levels of MMP-2, MMP-14 and Bcl-2	25667663
HL-60 AAA-Bcl-2	Apoptosis Assay	0-5 μM	48 h	IC50=0.87 μm，induces cell apoptosis in a dose-dependent manner	25711460
HL-60 EEE-Bcl-2	Apoptosis Assay	0-5 μM	48 h	IC50=5 μm， induces cell apoptosis in a dose-dependent manner	25711460
U937	Apoptosis Assay	0.5 μM	24 h	enhances cleavage of PARP and caspase-3 as well as Noxa level	25714024
U937	Apoptosis Assay	0.125-2 μM	24 h	enhances DHA/X-11-induced apoptosis	25714024
HCT116 BAX BAK1 DKO	Autophagy Assay	10 μM	12 h	induces a complete autophagic response	25715028
HCT116 BAX BAK1 DKO	Function Assay	10 μM	12 h	increases GFP-LC3B puncta	25715028
HCT116	Autophagy Assay	10 μM	12 h	induces a complete autophagic response	25715028
HCT116	Function Assay	10 μM	12 h	increases GFP-LC3B puncta	25715028
HCT116 BAX BAK1 DKO	Function Assay	3/10 μM	12 h	induces a dose-dependent increase in LC3B-II conversion and SQSTM1 degradation	25715028
HCT116	Function Assay	3/10 μM	12 h	induces a dose-dependent increase in LC3B-II conversion and SQSTM1 degradation	25715028
MM.1s	Apoptosis Assay	0-1.6 μM	24 h	induces cell apoptosis	25893290
MWCL-1	Apoptosis Assay	0-1.6 μM	24 h	induces cell apoptosis	25893290
BCWM.1	Apoptosis Assay	0-1.6 μM	24 h	induces cell apoptosis	25893290
B16	Cell Viability Assay	100 nM	72 h	enhances curcumin-induced anti-survival	26116776
WM-115	Cell Viability Assay	100 nM	72 h	enhances curcumin-induced anti-survival	26116776
LOUCY	Growth Inhibition Assay	100-1000 nM	48 h	IC50=32.8±10.9 nM	26172269
JURKAT	Growth Inhibition Assay	100-1000 nM	48 h	IC50=955±9.3 nM	26172269
CEM S	Apoptosis Assay	10-1000 nM	24 h	causes the cleavage of Bcl-2 and the downregulation of Bcl-xL and Mcl-1	26392332
MOLT-4	Apoptosis Assay	10-1000 nM	24 h	causes the cleavage of Bcl-2 and the downregulation of Bcl-xL and Mcl-1	26392332
CEM S	Growth Inhibition Assay	10-5000 nM	72 h	IC50=12.1 μM	26392332
CEM R	Growth Inhibition Assay	10-5000 nM	72 h	IC50=5.4 μM	26392332
JURKAT	Growth Inhibition Assay	10-5000 nM	72 h	IC50=66 μM	26392332
RS4;11	Growth Inhibition Assay	10-5000 nM	72 h	IC50=0.002 μM	26392332
MOLT-4	Growth Inhibition Assay	10-5000 nM	72 h	IC50=0.198 μM	26392332
MC-3	Apoptosis Assay	5/10/20 μM	24 h	induces caspase-mediated apoptosis	26447615
HN22	Apoptosis Assay	2.5/7.5/22.5 μM	24 h	induces caspase-mediated apoptosis	26447615
HN22	Growth Inhibition Assay	2.5/7.5/22.5 μM	24 h	inhibits cell growth in a dose-dependent manner	26447615
MC-3	Growth Inhibition Assay	5/10/20 μM	24 h	inhibits cell growth in a dose-dependent manner	26447615
Kasumi-1	Apoptosis Assay	0-10 μM	24 h	induces cell apoptosis in a dose-dependent manner	26552712
KG1a	Apoptosis Assay	0-10 μM	24 h	induces cell apoptosis in a dose-dependent manner	26552712
Kasumi-1	Cell Viability Assay	0-10 μM	24 h	IC50=4.87 μM, decreases cell viability in a dose-dependent manner	26552712
KG1a	Cell Viability Assay	0-10 μM	24 h	IC50=7.68 μM, decreases cell viability in a dose-dependent manner	26552712
OCI-Ly1	Cell Viability Assay	250 nM	72 h	caused 97% loss of viability in cells transfected with BCL6 siRNA	26657288
Eu-Myc	Apoptosis assay	1 uM		Induction of apoptosis in mouse Eu-Myc cells overexpressing BCL2 assessed as inhibition of colony formation at 1 uM	18040043
KB	Cytotoxicity assay	0.5 uM		Cytotoxicity in human siRNA-mediated-MCL1-kncok down KB cells overexpressing BCL2 at 0.5 uM	18040043
HCT116	Apoptosis assay		48 hrs	Induction of apoptosis in human HCT116 p53+/+ cells after 48 hrs by Annexin V-FITC staining-based flow cytometric method	26982372
BL21 (DE3)	Function assay		2 hrs	Binding affinity to N-terminus 8X His-tagged human Bcl-xL expressed in Escherichia coli BL21 (DE3) cells after 2 hrs by fluorescence polarization assay, Ki = 0.001 μM.	22448988
BL21 (DE3)	Function assay		2 hrs	Binding affinity to N-terminus 6X His-tagged human Bcl2 expressed in Escherichia coli BL21 (DE3) cells after 2 hrs by fluorescence polarization assay, Ki = 0.0006 μM.	22448988
Remb1	Cytotoxicity assay		24 hrs	Cytotoxicity against human Remb1 cells assessed as reduction in cell viability after 24 hrs by MTT assay, IC50 = 1.4 μM.	29453135
RS4:11	Cytotoxicity assay		24 hrs	Cytotoxicity against human RS4:11 cells assessed as reduction in cell viability after 24 hrs by MTT assay, IC50 = 0.33 μM.	29453135
SKOV3	Growth inhibition assay		72 hrs	Growth inhibition of human SKOV3 cells after 72 hrs by MTT assay, IC50 = 46.59 μM.	27712939
U266	Growth inhibition assay		72 hrs	Growth inhibition of human U266 cells after 72 hrs by MTT assay, IC50 = 27.35 μM.	27712939
MCF7	Growth inhibition assay		72 hrs	Growth inhibition of human MCF7 cells after 72 hrs by MTT assay, IC50 = 25.33 μM.	27712939
HL60	Growth inhibition assay		72 hrs	Growth inhibition of human HL60 cells after 72 hrs by MTT assay, IC50 = 0.97 μM.	27712939
NCI-H1417	Cytotoxicity assay		4 days	Cytotoxicity against human NCI-H1417 cells assessed as growth inhibition after 4 days by WST assay, IC50 = 0.1734 μM.	23448298
NCI-H187	Cytotoxicity assay		4 days	Cytotoxicity against human NCI-H187 cells assessed as growth inhibition after 4 days by WST assay, IC50 = 0.1377 μM.	23448298
NCI-H1963	Cytotoxicity assay		4 days	Cytotoxicity against human NCI-H1963 cells assessed as growth inhibition after 4 days by WST assay, IC50 = 0.054 μM.	23448298
K562	Apoptosis assay		48 hrs	Induction of apoptosis in Mcl1 dependent human K562 cells after 48 hrs by Annexin V staining based flow cytometry, IC50 = 16.4 μM.	23314054
RS4:11	Apoptosis assay		48 hrs	Induction of apoptosis in Bcl2 dependent human RS4:11 cells after 48 hrs by Annexin V staining based flow cytometry, IC50 = 0.27 μM.	23314054
NCI-H1417	Antiproliferative assay		4 days	Antiproliferative activity against human NCI-H1417 cells after 4 days by WST8 assay, IC50 = 0.412 μM.	22747598
NCI-H1963	Antiproliferative assay		4 days	Antiproliferative activity against human NCI-H1963 cells after 4 days by WST8 assay, IC50 = 0.059 μM.	22747598
NCI-H146	Antiproliferative assay		4 days	Antiproliferative activity against human NCI-H146 cells after 4 days by WST8 assay, IC50 = 0.037 μM.	22747598
K562	Cytotoxicity assay		48 hrs	Cytotoxicity against human K562 cells assessed as cell viability after 48 hrs by celltiter-blue assay, IC50 = 34.7 μM.	22582991
HL60	Cytotoxicity assay		48 hrs	Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by celltiter-blue assay, IC50 = 0.76 μM.	22582991
CCRF-CEM	Cytotoxicity assay		48 hrs	Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay, IC50 = 0.74 μM.	22582991
NCI-H1417	Growth inhibition assay		4 days	Growth inhibition of human NCI-H1417 cells after 4 days by WST8 assay, IC50 = 0.13 μM.	22448988
NCI-H146	Growth inhibition assay		4 days	Growth inhibition of human NCI-H146 cells after 4 days by WST8 assay, IC50 = 0.097 μM.	22448988
BL21 (DE3)	Function assay		2 hrs	Binding affinity to N-terminus 8X His-tagged human Bcl-xL expressed in Escherichia coli BL21 (DE3) cells after 2 hrs by fluorescence polarization assay, IC50 = 0.006 μM.	22448988
BL21 (DE3)	Function assay		2 hrs	Binding affinity to N-terminus 6X His-tagged human Bcl2 expressed in Escherichia coli BL21 (DE3) cells after 2 hrs by fluorescence polarization assay, IC50 = 0.002 μM.	22448988
HCT116	Cytotoxicity assay		72 hrs	Cytotoxicity against human HCT116 cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay, IC50 = 47.7 μM.	22172701
DU145	Cytotoxicity assay		48 hrs	Cytotoxicity against human DU145 cells after 48 hrs by cell titer-blue assay, IC50 = 27.6 μM.	19743858
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells after 48 hrs by cell titer-blue assay, IC50 = 21.26 μM.	19743858
Hepa-1c1c7	Cytotoxicity assay		48 hrs	Cytotoxicity against mouse Hepa-1c1c7 cells after 48 hrs by cell titer-blue assay, IC50 = 8.68 μM.	19743858
H460	Cytotoxicity assay		48 hrs	Cytotoxicity against human H460 cells after 48 hrs by cell titer-blue assay, IC50 = 8.03 μM.	19743858
SU-8686	Cytotoxicity assay		48 hrs	Cytotoxicity against human SU-8686 cells after 48 hrs by cell titer-blue assay, IC50 = 4.24 μM.	19743858
HCT116	Cytotoxicity assay		48 hrs	Cytotoxicity against human HCT116 cells after 48 hrs by cell titer-blue assay, IC50 = 4.06 μM.	19743858
Jurkat	Cytotoxicity assay		48 hrs	Cytotoxicity against human Jurkat cells after 48 hrs by cell titer-blue assay, IC50 = 1.38 μM.	19743858
MEF	Cytotoxicity assay		24 hrs	Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% fetal bovine serum, EC50 = 0.051 μM.	21366295
MEF	Cytotoxicity assay		24 hrs	Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% serum, EC50 = 0.051 μM.	21366295
MEF	Cytotoxicity assay		24 hrs	Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 1% serum, EC50 = 0.00203 μM.	21366295
NCI-H146	Cytotoxicity assay		48 hrs	Cytotoxicity against human NCI-H146 cells assessed as cell viability after 48 hrs in presence of 10% human serum, EC50 = 0.087 μM.	18841882
FL5.12	Cytotoxicity assay		24 hrs	Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl-XL assessed as cell viability after 24 hrs by MTS assay in absence of serum, EC50 = 0.03 μM.	18841882
FL5.12	Cytotoxicity assay		24 hrs	Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl2 assessed as cell viability after 24 hrs by MTS assay in absence of serum, EC50 = 0.0077 μM.	18841882
UPCI:SCC90	Growth Inhibition Assay		72 h	GI50=6.6 ± 1.5 μM	25139387
UD-SCC2	Growth Inhibition Assay		72 h	GI50=28 ± 2.9 μM	25139387
93-VU-147T	Growth Inhibition Assay		72 h	GI50=4.3 ± 3.5 μM	25139387
UM-SCC47	Growth Inhibition Assay		72 h	GI50=19 ± 12.3 μM	25139387
UM-SCC22B	Growth Inhibition Assay		72 h	GI50=19 ± 2.9 μM	25139387
PCI-15B	Growth Inhibition Assay		72 h	GI50=11 ± 4.5 μM	25139387
PCI-13	Growth Inhibition Assay		72 h	GI50=15 ± 1.8 μM	25139387
OCI-AML3	Growth Inhibition Assay		72 h	IC50 = 1950 nM	26045609
MOLM-13	Growth Inhibition Assay		72 h	IC50 = 27.9 nM	26045609
HL-60	Growth Inhibition Assay		72 h	IC50 = 10.7 nM	26045609
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
Toledo	Apoptosis assay			Induction of apoptosis in human Toledo cells, LD50 = 0.06 μM.	24900652
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
MOLT4	Antiproliferative assay			Antiproliferative activity against human MOLT4 cells in presence of 10% human serum, EC50 = 0.622 μM.	28926247
RS4:11	Antiproliferative assay			Antiproliferative activity against human RS4:11 cells in presence of 10% human serum, EC50 = 0.024 μM.	28926247
CLL	Apoptosis assay			Induction of apoptosis in human CLL cells, EC50 = 0.0045 μM.	20925433
SUDHL4	Growth inhibition assay			Inhibition of cell growth in human SUDHL4 cells overexpressing Bcl2 in presence of 10% HS, EC50 = 0.85 μM.	17256834
FL5.12	Function assay			Reversal of cytokine withdrawal protection in IL3 dependent Bcl-xL overexpressing mouse FL5.12 cells in presence of 3% FBS, EC50 = 0.22 μM.	17256834
SUDHL4	Growth inhibition assay			Inhibition of cell growth in human SUDHL4 cells overexpressing Bcl2 in presence of 3% FBS, EC50 = 0.22 μM.	17256834
RS11380	Growth inhibition assay			Inhibition of cell growth in human RS11380 cells overexpressing Bcl2 in presence of 10% HS, EC50 = 0.15 μM.	17256834
DoHH2	Growth inhibition assay			Inhibition of cell growth in human DoHH2 cells overexpressing Bcl2 in presence of 10% HS, EC50 = 0.13 μM.	17256834
FL5.12	Function assay			Reversal of cytokine withdrawal protection in IL3 dependent Bcl2 overexpressing mouse FL5.12 cells in presence of 3% FBS, EC50 = 0.05 μM.	17256834
FL5.12	Function assay			Reversal of cytokine withdrawal protection in IL3 dependent Bcl-xL overexpressing mouse FL5.12 cells in presence of bovine gelatin, EC50 = 0.03 μM.	17256834
DoHH2	Growth inhibition assay			Inhibition of cell growth in human DoHH2 cells overexpressing Bcl2 in presence of 3% FBS, EC50 = 0.0083 μM.	17256834
RS11380	Growth inhibition assay			Inhibition of cell growth in human RS11380 cells overexpressing Bcl2 in presence of 3% FBS, EC50 = 0.014 μM.	17256834
FL5.12	Function assay			Reversal of cytokine withdrawal protection in IL3 dependent Bcl2 overexpressing mouse FL5.12 cells in presence of bovine gelatin, EC50 = 0.008 μM.	17256834
U266	Growth Inhibition Assay			IC50=0.68 μM	25535900
NCI-H929	Growth Inhibition Assay			IC50=15.21 μM	25535900
MM.1S	Growth Inhibition Assay			IC50=0.40 μM	25535900
RPMI 8226	Growth Inhibition Assay			IC50=0.25 μM	25535900
U937	Growth Inhibition Assay			IC50=5.29 μM	25535900
C1498	Growth Inhibition Assay			IC50=6.13 μM	25535900
THP-1	Growth Inhibition Assay			IC50=1.27 μM	25535900
Kasumi-1	Growth Inhibition Assay			IC50=0.01 μM	25535900
Kasumi-1/ABT	Growth Inhibition Assay			IC50=0.51 μM	25535900
JurkatΔBak	Growth Inhibition Assay			IC50>50 μM	25535900
HL60/VCR	Growth Inhibition Assay			IC50>100 μM	25535900
K562/Bcl- 2-IRESBim	Growth Inhibition Assay			IC50=0.35 μM	25535900
Jurkat	Growth Inhibition Assay			IC50=0.66 μM	25535900
K562/Mcl -1-IRESBim	Growth Inhibition Assay			IC50=9.3 μM	25535900
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
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生物活性

製品説明

特性

First-generation inhibitor of anti-apoptotic Bcl-2 proteins.

Targets

Bcl-2 ^[1] (Cell-free assay)	Bcl-xL ^[1] (Cell-free assay)	Bcl-w ^[1] (Cell-free assay)	Bcl-B ^[1] (Cell-free assay)
30.3 nM(EC50)	78.7 nM(EC50)	197.8 nM(EC50)	1.82 μM(EC50)

In Vitro
In vitro	ABT-737 shows low activity to Bcl-B and no effects to Mcl-1 and BFL-1. ABT-737 is sensitive to HL60, KG1 and NB4 cells with IC50 of 50 nM, 80 nM and 80 nM, respectively. ABT-737 induces apoptosis in HL60 cells, which due to decreased Bcl-2/Bax heterodimerization and has no effect on cell cycle distribution. ABT-737 also induces cytochrome c release from purified mitochondria and promotes conformational changes in Bax that are associated with apoptosis. ^[1] Resistant cells (Hela and MCF-7) can be sensitized to ABT-737 by approaches that down-regulate, destabilize, or inactivate Mcl-1. ABT-737 also causes Bax/BAK-dependent cytochrome c release only when Mcl-1 has been neutralized. ^[2] ABT-737 displaces Bim from Bcl2's BH3-binding pocket, allowing Bim to activate Bax, induce mitochondrial permeabilization, and rapidly commit the primary chronic lymphocytic leukemia (CLL) cells to death. ^[3] Knockdown of Mcl-1 with siRNA sensitizes two resistant SCLC cell lines H196 and DMS114 to ABT-737 by enhancing the induction of apoptosis. Likewise, up-regulation of Noxa sensitizes H196 cells to ABT-737. ABT-737 inhibits proliferation and induces apoptosis in many SCLC cell lines including NCI-H889, NCI-H1963, NCI-H1417, NCI-H146 and etc. Bcl-2 and Noxa may contribute mechanistically to the cellular response to ABT-737 in NCI-H146 cells. ^[4] A recent study shows that ABT-737 significantly induces apoptosis in HTLV-1 infected T-cell lines as well as in fresh ATLL cells. ^[5]
Kinase Assay	Fluorescence polarization assays
Kinase Assay	Binding affinity of GST-Bcl-2 family proteins to the FITC-conjugated BH3 domain of Bim (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR) is determined. Briefly, 100 nM of GST-Bcl-2 family fusion proteins are incubated with serial dilutions of ABT-737 in PBS for 2 min. Then, 20 nM of FITC-Bim BH3 peptide (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR) is added. Fluorescence polarization is measured using an Analyst TM AD Assay Detection System after 10 min using the 96-well black plate. Then IC50 are determined.
細胞実験	細胞株	SCLC cell lines NCI-H889, NCI-H1963, NCI-H1417, NCI-H146, NCI-187, DMS79, NCI-1048, NCI-H82, NCI-H196, H69AR, and DMS114
	濃度	0.001-10 μM
	反応時間	48 hours
	実験の流れ	SCLC cells are treated for 48 hours in 96-well tissue culture plates in a total volume of 100 μL tissue culture medium supplemented with 10% human serum. Viable cells are determined using the MTS assay.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	γ-H2AX / p-ATM Hif-1a PARP / c-PARP / cleaved caspase 3		21084274
	Immunofluorescence	p65 AIF Bim Bax cytochrome C		28846096
	Growth inhibition assay	Cell viability		22311987
	ELISA	IL-6 / IL-8		21084274

In Vivo
In Vivo	In aggressive leukemia model, ABT-737 suppresses the leukemia burden by 53% at the 30 mg/kg, with significantly extended survival of mice. ABT-737 does not induce significantly abnormalities in blood cell counts or serum chemistries. ^[1] ABT-737 prolongs the survival of recipient mice transplanted with Bcl-2-transduced tumors. ^[2] ABT-737 shows great antitumor activity in an ATLL mouse model at a dose of 100 mg/kg. ^[5]
動物実験	動物モデル	Scid mice injected with Luc-expressing FD/ΔRaf-1:ER cells
	投与量	20 and 30 mg/kg
	投与経路	For intraperitoneal (i.p.) every day

参考
[1] Konopleva M, et al. Cancer Cell, 2006, 10(5), 375-388. [2] van Delft MF,et al. Cancer Cell, 2006, 10(5), 389-399. [3] Del Gaizo Moore V, et al. J Clin Invest, 2007, 117(1), 112-121. [4] Tahir SK, et al. Cancer Res, 2007, 67(3), 1176-1183. [5] Ishitsuka K, et al. Cancer Lett, 2012, 317(2), 218-225. [6] Konopleva M, et al. Cancer Res, 2008, 68(9), 3413-3420. [7] Wade M, et al. Cell Cycle, 2008, 7(13), 1973-1982. [8] Paoluzzi L, et al. Blood, 2008, 112(7), 2906-2916. [9] Li R, et al. Mol Pharmacol, 2009, 75(5), 1231-1239. + 展開

参考

+ 展開

化学情報

分子量	813.43	化学式	C₄₂H₄₅ClN₆O₅S₂
CAS No.	852808-04-9	SDF	Download ABT-737 SDFをダウンロードする
Smiles	CN(C)CCC(CSC1=CC=CC=C1)NC2=C(C=C(C=C2)S(=O)(=O)NC(=O)C3=CC=C(C=C3)N4CCN(CC4)CC5=CC=CC=C5C6=CC=C(C=C6)Cl)[N+](=O)[O-]
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个月-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (122.93 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:
What’s the recommended method about reconstitution of the compound for in vivo animal study?

回答
For oral administration, we suggest the vehicle: 30% Propylene glycol, 5% Tween 80, 65% D5W, at up to 30mg/ml; For injection, ABT-737 can be dissolved in 2% DMSO/50% PEG 300/5% Tween 80/ddH2O at 2.5 mg/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):