产品名称

Venetoclax

一般描述

Venetoclax is a Bcl-2-selective inhibitor.

别 称

ABT-199, GDC-0199

纯 度

≥99.0%(HPLC)

CAS NO.

1257044-40-8

分子式

C⁴⁵H⁵⁰ClN⁷O⁷S

分子量

868.44

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

浅黄色至黄色或橙黄色粉末

溶解性(25℃)

DMSO

≥50mg/mL(warmed)

乙醇

Insoluble

水

Insoluble

l  生物学信息

生物活性/药理作用

Venetoclax is an orally bioavailable, selective small molecule inhibitor of the anti-apoptotic protein Bcl-2, with potential antineoplastic activity. Venetoclax mimics BH3-only proteins, the native ligands of Bcl-2 and apoptosis activators, by binding to the hydrophobic groove of Bcl-2 proteins thereby repressing Bcl-2 activity and restoring apoptotic processes in tumor cells. Bcl-2 protein is overexpressed in some cancers and plays an important role in the regulation of apoptosis; its  is associated with increased drug resistance and tumor cell survival. Compared to the Bcl-2 inhibitor navitoclax, this agent does not  inhibit bcl-XL and does not cause bcl-XL-mediated thrombocytopenia.

Venetoclax is a Bcl-2-selective inhibitor with Ki of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1.

l  存储

存储温度

-20℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov