|(R)-4-(4-((4'-氯-[1,1'-联苯]-2-基)甲基)哌嗪-1-基)-N-((4-((4-(二甲氨基)-1-(苯硫基)丁基-2-基)氨基)-3-硝基苯基)磺酰)苯甲酰胺|CsnPharm

CAS No.: 852808-04-9

ABT-737 Catalog No. CSN12426

Synonyms: ABT-737

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, respectively, showing no inhibition observed against Mcl-1, Bcl-B or Bfl-1.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Bcl-2

EC50:30.3nM Bcl-w

EC50:197.8nM Bcl-xL

EC50:78.7nM
描述The B-cell lymphoma 2 (Bcl-2) family of proteins is composed of both antiapoptotic members, such as Bcl-2, Bcl-xL as well as Bcl-w, and proapoptotic members. Up-regulation of the pro-survival Bcl-2 family proteins is one of the primary means for cancer cells to evade apoptosis. ABT-737 is a selective inhibitor of Bcl-2 family with EC50 values of 78.7nM, 30.3nM and 198.8nM for BCL-XL, BCL-2 and BCL-W (measured by FP assay), respectively, with almost no inhibition on BCL-B, BFL-1 and MCL-1. ABT-737 can inhibit cell growth with IC50 values of 50nM, 80nM, 80nM, 2μM and 5μM for leukemic cells HL60, KG1, NB4, U937 and OCI-AML3 cells, as well as and induce apoptosis at dose of 100nM for 12 or 24h in HL60. As a BH3 mimetic small-molecule, the in vitro studies showed that ABT-737 disrupted BCL-2/BAX heterodimerization and improved the apoptosis throuth inducing BAX change to a “prodeath'' conformation in AML cells. Both inhibition of BCL-2 phosphorylation and suppression of MCL-1 expression could enhance ABT-737-mediated apoptosis. Intraperitoneal administration of ABT-737 at dose of 20 and 30mg/kg suppressed the leukemia burden by 48% and 53%, respectively, as well as significantly extended survival of leukemia model. A similar inhibition of leukemia burden was also observed in a human xenograft leukemia model with KG-1 cells^[1].
作用机制ABT-737 is a BH3 mimetic small-molecule that can occupies the BH3 binding groove of BCL-2.^[1]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
93-VU-147T	-	Growth Inhibition Assay	72 h	GI50=4.3 ± 3.5 μM	25139387
A549	0-20 μM	Cell Viability Assay	72 h	decreases the cell survival in a dose-dependent manner combined with aspirin	25388762
A549	20 μM	Apoptosis Assay	48 h	induces apoptosis significantly combined with aspirin	25388762

更多
动物研究
剂量
Mice: min = 25 mg/kg^[2], max = 100 mg/kg^[3]

给药途径
i.p., i.v.
临床研究

动物研究
剂量	Mice: min = 25 mg/kg^[2], max = 100 mg/kg^[3]
给药途径	i.p., i.v.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01440504	-	-	Completed	-	France ... more >> Centre François Baclesse Caen, France, 14076 Collapse <<

参考文献

[1] Konopleva M, Contractor R, et al. Mechanisms of apoptosis sensitivity and resistance to the BH3 mimetic ABT-737 in acute myeloid leukemia. Cancer Cell. 2006;10(5):375-88.
[2] Whitecross KF, Alsop AE, et al. Defining the target specificity of ABT-737 and synergistic antitumor activities in combination with histone deacetylase inhibitors. Blood. 2009;113(9):1982-91.
[3] Jain HV, Richardson A, et al. Exploiting the synergy between carboplatin and ABT-737 in the treatment of ovarian carcinomas. PLoS One. 2014;9(1):e81582.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.2294 mL
- 6.1468 mL
- 12.2936 mL
- 5 mM
- 0.2459 mL
- 1.2294 mL
- 2.4587 mL
- 10 mM
- 0.1229 mL
- 0.6147 mL
- 1.2294 mL

技术信息

CAS号

852808-04-9

储存条件

粉末: Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C42H45ClN6O5S2

运输

蓝冰

分子量

813.43

别名

ABT-737

溶解度

DMSO	140.0 mg/mL (172.1 mM)
Water	insoluble

动物实验配方

2%DMSO+40%PEG300+5%Tween80+53%water

2 mg/mL

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

93-VU-147T	-	Growth Inhibition Assay	72 h	GI50=4.3 ± 3.5 μM	25139387
A549	0-20 μM	Cell Viability Assay	72 h	decreases the cell survival in a dose-dependent manner combined with aspirin	25388762
A549	20 μM	Apoptosis Assay	48 h	induces apoptosis significantly combined with aspirin	25388762
A5-RT3	0.1/1/10 μM	Cell Viability Assay	24 h	decreases cell viability in a dose-dependent manner	25210795
A5-RT3	10 μM	Function Assay	24/48 h	induces MMP and DNA fragmentation	25210795
A5-RT3	5 μM	Function Assay	6 h	induces the release of mitochondrial proteins and reduces clonogenic survival in a caspase-independent manner	25210795
B16	100 nM	Cell Viability Assay	72 h	enhances curcumin-induced anti-survival	26116776
BCWM.1	0-1.6 μM	Apoptosis Assay	24 h	induces cell apoptosis	25893290
C1498	-	Growth Inhibition Assay	-	IC50=6.13 μM	25535900
Caco2	1/5/10 μM	Apoptosis Assay	48 h	causes cell death in a dose-dependent manner	25192188
Caco-2	0-10 μM	Cell Viability Assay	24 h	IC50=19.7 µM	25304383
CEM R	10-5000 nM	Growth Inhibition Assay	72 h	IC50=5.4 μM	26392332
CEM S	10-5000 nM	Growth Inhibition Assay	72 h	IC50=12.1 μM	26392332
CEM S	10-1000 nM	Apoptosis Assay	24 h	causes the cleavage of Bcl-2 and the downregulation of Bcl-xL and Mcl-1	26392332
Clone A	0.2–60 μM	Growth Inhibition Assay	72 h	IC50=7.5 μM	25208882
COG-LL-319	100 nM	Function Assay	1/3/6 h	induces caspase-dependent Mcl-1 cleavage	24951472
Colo205	1/5/10 μM	Apoptosis Assay	48 h	causes cell death in a dose-dependent manner	25192188
CX-1	0.2–60 μM	Growth Inhibition Assay	72 h	IC50=1.8 μM	25208882
DLD1	0-10 μM	Cell Viability Assay	24 h	IC50=18.78 µM	25304383
H1299	0-20 μM	Cell Viability Assay	72 h	decreases the cell survival in a dose-dependent manner combined with aspirin	25388762
H1299	20 μM	Apoptosis Assay	48 h	induces apoptosis significantly combined with aspirin	25388762
HaCaT	0.1/1/10 μM	Cell Viability Assay	24 h	decreases cell viability in a dose-dependent manner	25210795
HaCaT	10 μM	Function Assay	24/48 h	induces MMP and DNA fragmentation	25210795
HCT116	3/10 μM	Function Assay	12 h	induces a dose-dependent increase in LC3B-II conversion and SQSTM1 degradation	25715028
HCT116	10 μM	Function Assay	12 h	increases GFP-LC3B puncta	25715028
HCT116	10 μM	Autophagy Assay	12 h	induces a complete autophagic response	25715028
HCT116	0-10 μM	Cell Viability Assay	24 h	IC50=20.49 µM	25304383
HCT-116	0-20 μM	Cell Viability Assay	72 h	decreases the cell survival in a dose-dependent manner combined with aspirin	25388762
HCT116 BAX BAK1 DKO	3/10 μM	Function Assay	12 h	induces a dose-dependent increase in LC3B-II conversion and SQSTM1 degradation	25715028
HCT116 BAX BAK1 DKO	10 μM	Function Assay	12 h	increases GFP-LC3B puncta	25715028
HCT116 BAX BAK1 DKO	10 μM	Autophagy Assay	12 h	induces a complete autophagic response	25715028
HL-60	-	Growth Inhibition Assay	72 h	IC50 = 10.7 nM	26045609
HL-60 AAA-Bcl-2	0-5 μM	Apoptosis Assay	48 h	IC50=0.87 μm，induces cell apoptosis in a dose-dependent manner	25711460
HL-60 EEE-Bcl-2	0-5 μM	Apoptosis Assay	48 h	IC50=5 μm， induces cell apoptosis in a dose-dependent manner	25711460
HL60/VCR	-	Growth Inhibition Assay	-	IC50>100 μM	25535900
HN22	2.5/7.5/22.5 μM	Growth Inhibition Assay	24 h	inhibits cell growth in a dose-dependent manner	26447615
HN22	2.5/7.5/22.5 μM	Apoptosis Assay	24 h	induces caspase-mediated apoptosis	26447615
HO-8910	0-20 μM	Cell Viability Assay	72 h	decreases the cell survival in a dose-dependent manner combined with aspirin	25388762
HT29	1/5/10 μM	Apoptosis Assay	48 h	causes cell death in a dose-dependent manner	25192188
HT-29	0-20 μM	Cell Viability Assay	72 h	decreases the cell survival in a dose-dependent manner combined with aspirin	25388762
JURKAT	10-5000 nM	Growth Inhibition Assay	72 h	IC50=66 μM	26392332
JURKAT	100-1000 nM	Growth Inhibition Assay	48 h	IC50=955±9.3 nM	26172269
Jurkat	-	Growth Inhibition Assay	-	IC50=0.66 μM	25535900
JurkatΔBak	-	Growth Inhibition Assay	-	IC50>50 μM	25535900
K562	1-10 μM	Cell Viability Assay	48 h	IC50=26.7 μM	25596561
K562/Bcl- 2-IRESBim	-	Growth Inhibition Assay	-	IC50=0.35 μM	25535900
K562/Mcl -1-IRESBim	-	Growth Inhibition Assay	-	IC50=9.3 μM	25535900
Kasumi-1	0-10 μM	Cell Viability Assay	24 h	IC50=4.87 μM, decreases cell viability in a dose-dependent manner	26552712
Kasumi-1	0-10 μM	Apoptosis Assay	24 h	induces cell apoptosis in a dose-dependent manner	26552712
Kasumi-1	-	Growth Inhibition Assay	-	IC50=0.01 μM	25535900
Kasumi-1/ABT	-	Growth Inhibition Assay	-	IC50=0.51 μM	25535900
KG1a	0-10 μM	Cell Viability Assay	24 h	IC50=7.68 μM, decreases cell viability in a dose-dependent manner	26552712
KG1a	0-10 μM	Apoptosis Assay	24 h	induces cell apoptosis in a dose-dependent manner	26552712
LOUCY	100-1000 nM	Growth Inhibition Assay	48 h	IC50=32.8±10.9 nM	26172269
LS174T	0.2–60 μM	Growth Inhibition Assay	72 h	IC50=18.3 μM	25208882
LS411N	0-10 μM	Cell Viability Assay	24 h	IC50=11.47 µM	25304383
MC-3	5/10/20 μM	Growth Inhibition Assay	24 h	inhibits cell growth in a dose-dependent manner	26447615
MC-3	5/10/20 μM	Apoptosis Assay	24 h	induces caspase-mediated apoptosis	26447615
MCF-7	5 μM	Cell Viability Assay	48 h	enhances the sensitivity to or radiation	25409124
MCF-7	5 μM	Apoptosis Assay	4/24/48 h	increases the cleaved PARP	25409124
MCF-7	5 μM	Function Assay	24 h	enhances thelevel of Mcl-1 expression	25409124
MDA-MB 231	5 μM	Function Assay	24 h	enhances thelevel of Mcl-1 expression	25409124
MM.1s	0-1.6 μM	Apoptosis Assay	24 h	induces cell apoptosis	25893290
MM.1S	-	Growth Inhibition Assay	-	IC50=0.40 μM	25535900
MM.1S	500/750 nM	Function Assay	24/48 h	downregulates Bim, principally the EL isoform	25208888
MOLM-13	-	Growth Inhibition Assay	72 h	IC50 = 27.9 nM	26045609
MOLT-4	10-5000 nM	Growth Inhibition Assay	72 h	IC50=0.198 μM	26392332
MOLT-4	10-1000 nM	Apoptosis Assay	24 h	causes the cleavage of Bcl-2 and the downregulation of Bcl-xL and Mcl-1	26392332
MWCL-1	0-1.6 μM	Apoptosis Assay	24 h	induces cell apoptosis	25893290
NCI-H929	-	Growth Inhibition Assay	-	IC50=15.21 μM	25535900
OCI-AML3	-	Growth Inhibition Assay	72 h	IC50 = 1950 nM	26045609
OCI-Ly1	250 nM	Cell Viability Assay	72 h	caused 97% loss of viability in cells transfected with BCL6 siRNA	26657288
OcI-LY18	0.0001-1 μM	Cell Viability Assay	96 h	decreases the cell viability in a dose-dependent manner	25373508
OPM-2	125/250/500 nM	Cell Viability Assay	48h	decreases cell viability in a dose-dependent manner	25008202
OPM-2	125/250/500 nM	Apoptosis Assay	48h	induces cell apoptosis in a dose-dependent manner	25008202
PCI-13	-	Growth Inhibition Assay	72 h	GI50=15 ± 1.8 μM	25139387
PCI-15B	-	Growth Inhibition Assay	72 h	GI50=11 ± 4.5 μM	25139387
RKO	0-10 μM	Cell Viability Assay	24 h	IC50> 25 µM	25304383
RL	0.0001-1 μM	Cell Viability Assay	96 h	decreases the cell viability in a dose-dependent manner	25373508
RPMI 8226	-	Growth Inhibition Assay	-	IC50=0.25 μM	25535900
RPMI8226	500/750 nM	Function Assay	24/48 h	downregulates Bim, principally the EL isoform	25208888
RPMI-8226	125/250/500 nM	Cell Viability Assay	48h	decreases cell viability in a dose-dependent manner	25008202
RPMI-8226	125/250/500 nM	Apoptosis Assay	48h	induces cell apoptosis in a dose-dependent manner	25008202
RS4;11	10-5000 nM	Growth Inhibition Assay	72 h	IC50=0.002 μM	26392332
RS4;11	100 nM	Function Assay	1/3/6 h	induces caspase-dependent Mcl-1 cleavage	24951472
Sc-1	0.0001-1 μM	Cell Viability Assay	96 h	decreases the cell viability in a dose-dependent manner	25373508
SW480	1/5/10 μM	Apoptosis Assay	48 h	causes cell death in a dose-dependent manner	25192188
SW620	0-10 μM	Cell Viability Assay	24 h	IC50=12.24 µM	25304383
THP-1	-	Growth Inhibition Assay	-	IC50=1.27 μM	25535900
U266	-	Growth Inhibition Assay	-	IC50=0.68 μM	25535900
U266	500/750 nM	Function Assay	24/48 h	downregulates Bim, principally the EL isoform	25208888
U87	50 μM	Function Assay	24 h	reduces the mRNA expression levels of MMP-2, MMP-14 and Bcl-2	25667663
U937	0.125-2 μM	Apoptosis Assay	24 h	enhances DHA/X-11-induced apoptosis	25714024
U937	0.5 μM	Apoptosis Assay	24 h	enhances cleavage of PARP and caspase-3 as well as Noxa level	25714024
U937	-	Growth Inhibition Assay	-	IC50=5.29 μM	25535900
UD-SCC2	-	Growth Inhibition Assay	72 h	GI50=28 ± 2.9 μM	25139387
UM-SCC22B	-	Growth Inhibition Assay	72 h	GI50=19 ± 2.9 μM	25139387
UM-SCC47	-	Growth Inhibition Assay	72 h	GI50=19 ± 12.3 μM	25139387
UPCI:SCC90	-	Growth Inhibition Assay	72 h	GI50=6.6 ± 1.5 μM	25139387
WM-115	100 nM	Cell Viability Assay	72 h	enhances curcumin-induced anti-survival	26116776
ZR-75-1	5 μM	Function Assay	24 h	enhances thelevel of Mcl-1 expression	25409124

ABT-737 Catalog No. CSN12426

靶点选择性

请登录您的专属账户

确认信息