H3B-5942 ( H3B5942 )

产品货号. M13184 CAS No. 2052128-15-9

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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产品名称

H3B-5942
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

H3B-5942 is an orally available, selective estrogen receptor covalent antagonist (SERCA), demonstrates potent ERαantagonist activity in vitro and in vivo.
产品描述

H3B-5942 is an orally available, selective estrogen receptor covalent antagonist (SERCA), demonstrates potent ERαantagonist activity in vitro and in vivo; covalently inactivates both wild-type and mutant ERα by targeting Cys530 and enforcing a unique antagonist conformation; demonstrated significant single-agent antitumor activity in xenograft models representing ERαWT and ERα Y537S breast cancer that was superior to fulvestrant.
同义词

H3B5942
通路

Endocrinology/Hormones
靶点

Estrogen Receptor/ERR
受体

Estrogen Receptor/ERR
研究领域

——
适应症

——

CAS Number

2052128-15-9
分子量

494.64
分子式

C31H34N4O2
纯度

>98% (HPLC)
溶解度

——
SMILES

CCC(=C(C1=CC=C(C=C1)OCCNCC=CC(=O)N(C)C)C2=CC3=C(C=C2)NN=C3)C4=CC=CC=C4
化学全称

(E)-4-((2-(4-((E)-1-(1H-indazol-5-yl)-2-phenylbut-1-en-1-yl)phenoxy)ethyl)amino)-N,N-dimethylbut-2-enamide

1. Puyang X, et al. Cancer Discov. 2018 Jul 10. pii: CD-17-1229.

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