ABT-737 | Bcl-2 Family Inhibitor/BH3 Mimetic | AmBeed-信号通路专用抑制剂

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ABT-737 99%+

货号：A821402

ABT-737 是一种选择性的 Bcl-2 家族蛋白抑制剂，能够有效抑制 Bcl-2、Bcl-xL 和 Bcl-w 的活性，IC50 值分别为 30.3 nM、78.7 nM 和 197.8 nM。ABT-737 主要用于研究细胞凋亡、抗癌治疗和增强肿瘤对化疗药物的敏感性。

ABT-737 化学结构
CAS号：852808-04-9

ABT-737 3D分子结构
CAS号：852808-04-9

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ABT-737 纯度/质量文件产品仅供科研

货号：A821402 标准纯度： 99%+ 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

Bcl-2 亚型比较
自噬亚型比较

产品名称	Bax ↓ ↑	Bcl-2 ↓ ↑	Bcl-B ↓ ↑	Bcl-w ↓ ↑	Bcl-xL ↓ ↑	Bfl-1 ↓ ↑	Mcl-1 ↓ ↑	其他靶点	纯度
BTSA1	✔								99%+
HA14-1		+ Bcl-2, IC50: 9 μM							98%
Venetoclax		++++ Bcl-2, Ki: <0.01 nM							99%
Navitoclax									99%+
Obatoclax Mesylate		+++ Bcl-2, Ki: 0.22 μM							98%
ABT-737		+++ Bcl-2, EC50: 30.3 nM	+ Bcl-B, EC50: 1.82 μM	+++ Bcl-w, EC50: 197.8 nM	+++ Bcl-xL, EC50: 78.7 nM				99%+
Gambogic Acid		+ Bcl-2, IC50: 1.21 μM Bfl-1, IC50: 1.06 μM	++ Bcl-B, IC50: 0.66 μM	++++ Bcl-w, IC50: 0.02 μM	+ Bcl-xL, IC50: 1.47 μM	+ Bfl-1, IC50: 1.06 μM	++ Mcl-1, IC50: 0.79 μM	Caspase	99% HPLC
BH3I-1					+ BH3-Bcl-xL interaction, Ki: 2.4 μM				98%
A-1331852					++++ Bcl-xL, Ki: <0.01 nM				99%+
A-1210477							++++ MCL-1, IC50: 26.2 nM		99%+
Maritoclax							✔		97%
TW-37		+++ Bcl-2, Ki: 0.29 μM			+ Bcl-xL, Ki: 1.11 μM		+++ Mcl-1, Ki: 0.26 μM		98%
UMI-77							++ Mcl-1, Ki: 490 nM		97%
(R)-(-)-Gossypol acetic acid		++ Bcl-2, Ki: 0.32 μM			++ Bcl-xL, Ki: 0.48 μM		+++ Mcl-1, Ki: 0.18 μM		98%
Sabutoclax		++ Bcl-2, IC50: 0.32 μM Bfl-1, IC50: 0.62 μM			++ Bcl-xL, IC50: 0.31 μM	++ Bfl-1, IC50: 0.62 μM	+++ Mcl-1, IC50: 0.20 μM		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	Autophagy ↓ ↑	其他靶点	纯度
SBI-0206965	+++ ULK2, IC50: 711 nM ULK1, IC50: 108 nM		97%
Hydroxychloroquine sulfate	✔		99%
Valproic acid sodium	✔	HDAC	97%
PFK-015	++ PFKFB3, IC50: 207 nM		99%+
MRT68921 hydrochloride	++++ ULK2, IC50: 1.1 nM ULK1, IC50: 2.9 nM		99%+
ROC-325	✔		99%+
Autophinib	+++ Autophagy, IC50: 40 nM		97%
Lys05	✔		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

ABT-737 生物活性

靶点	Bcl-xL Bcl-xL, EC50:78.7 nM Bcl-B Bcl-B, EC50:1.82 μM Bcl-w Bcl-w, EC50:197.8 nM Bcl-2 Bcl-2, EC50:30.3 nM
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]

ABT-737 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
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

ABT-737 动物研究

Dose	Mice: min = 25 mg/kg^[2], max = 100 mg/kg^[3]
Administration	i.p., i.v.

ABT-737 临床研究

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 ... 展开 >> Centre François Baclesse Caen, France, 14076 收起 <<

ABT-737 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.

ABT-737 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.23mL

0.25mL

0.12mL

6.15mL

1.23mL

0.61mL

12.29mL

2.46mL

1.23mL

ABT-737 技术信息

CAS号	852808-04-9
分子式	C₄₂H₄₅ClN₆O₅S₂
分子量	813.427

别名
运输	蓝冰

存储条件

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

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 50 mg/mL(61.47 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

2%DMSO+40%PEG300+5%Tween80+53%water 2 mg/mL

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

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 99%+

ABT-737 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

ABT-737 质控信息

ABT-737 生物活性

ABT-737 细胞研究

ABT-737 动物研究

ABT-737 临床研究

ABT-737 参考文献

ABT-737 实验方案

ABT-737 技术信息

最近浏览的产品

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Bcl-xL	Bcl-xL, EC50:78.7 nM
Bcl-B	Bcl-B, EC50:1.82 μM
Bcl-w	Bcl-w, EC50:197.8 nM
Bcl-2	Bcl-2, EC50:30.3 nM

ABT-737 99%+

ABT-737 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

ABT-737 质控信息

ABT-737 生物活性

ABT-737 细胞研究

ABT-737 动物研究

ABT-737 临床研究

ABT-737 参考文献

ABT-737 实验方案

ABT-737 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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ABT-737 纯度/质量文件产品仅供科研