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首页-小分子抑制剂&激动剂-Apoptosis-Bcl-2-Venetoclax
Venetoclax

Chemical Structure : Venetoclax

CAS No.: 1257044-40-8

Venetoclax (ABT-199, GDC-0199, ABT199)

货号: PC-49764Not For Human Use, Lab Use Only.

Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with Ki value of <0.01 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Venetoclax (ABT-199, GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with Ki value of <0.01 nM.
Venetoclax (ABT-199) displays >4800-fold selectivity for Bcl-2 over Bcl-xL and Bcl-w, and displays no measurable activity at Mcl-1.
Venetoclax (ABT-199) potently induces apoptosis in FL5.12-BCL-2 cells (EC50=261 nM) and reduces tumor burden in chronic lymphocytic leukemia (CLL) primary samples (EC50 =3 nM).
Venetoclax (ABT-199 enhances efficacy of clinically relevant chemotherapy and immunotherapy drugs.
Venetoclax (ABT-199) exhibits binding to SARS-CoV-2 3C-like protease (3CLpro) active site in a virtual screen.
Venetoclax (ABT-199) reverses oxidative phosphorylation in acute myeloid leukemia cells (AML), in vitro and in vivo.

物理化学性质&存储条件

分子量 868.45
分子式 C45H50ClN7O7S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-((1H-pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((3-nitro-4-(((tetrahydro-2H-pyran-4-yl)methyl)amino)phenyl)sulfonyl)benzamide

参考文献

1. Souers AJ, et al. Nat Med. 2013 Feb;19(2):202-8.

2. Vogler M, et al. Br J Haematol. 2013 Oct;163(1):139-42.

3. Vandenberg CJ, et al. Blood. 2013 Mar 21;121(12):2285-8.

4. Vaillant F, et al. Cancer Cell. 2013 Jul 8;24(1):120-9.

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