产品名称

Brilanestrant

一般描述

Brilanestrant is a potent ER-α binder (ER-α, IC50 = 6.1 nM ER-β, IC50 = 8.8 nM), a full tranional antagonist with no agonism and displays good potency and efficacy in ER-α degradation (EC50 = 0.7 nM) and MCF-7 breast cancer cell viability (IC50 = 2.5 nM) assays with good selectivity over other nuclear hormone receptors.

别 称

GDC-0810, ARN-810

纯 度

≥98.5%(HPLC)

CAS NO.

1365888-06-7

分子式

C²⁶H²⁰ClFN²O²

分子量

446.9

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

固体

溶解性(25°C)

DMSO

≥50mg/ml

乙醇

≥50mg/ml

水

Very slightly soluble

l  生物学信息

生物活性/药理作用

Brilanestrant is an orally available, nonsteroidal selective estrogen receptor degrader (SERD), with potential antineoplastic activity. Upon oral administration, brilanestrant binds to the estrogen receptor and induces a conformational change that results in the degradation of the receptor. This may inhibit the growth and survival of ER-expressing cancer cells.

l  存储

存储温度

-20°C

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