THIQ 40 ( THIQ40 )

产品货号. M12721 CAS No. 1799430-91-3

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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产品名称

THIQ 40
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

THIQ 40 (THIQ40) is a potent, orally available ERα antagonist and selective estrogen receptor degrader (SERD) with IC50 of 17 nM (ERα binding) and 30 nM (ERα transcription), IC50 of 0.9 nM (ERα degradation).
产品描述

THIQ 40 (THIQ40) is a potent, orally available ERα antagonist and selective estrogen receptor degrader (SERD) with IC50 of 17 nM (ERα binding) and 30 nM (ERα transcription), IC50 of 0.9 nM (ERα degradation); potently inhibits insulin driven proliferation in MCF-7 cells with IC50 of 2.1 nM, downregulate ERα protein levels and inhibit MCF-7 proliferation in an estradiol-independent manner; demonstrated SERD activity at tolerated and efficacious exposures in vivo.
同义词

THIQ40
通路

Endocrinology/Hormones
靶点

Estrogen Receptor/ERR
受体

Estrogen Receptor/ERR
研究领域

——
适应症

——

CAS Number

1799430-91-3
分子量

427.54
分子式

C28H29NO3
纯度

>98% (HPLC)
溶解度

——
SMILES

CC(C)C1=CC=C(C=C1)N2CCC3=C(C2(C)C4=CC=C(C=C4)C=CC(=O)O)C=CC(=C3)O
化学全称

(E)-3-(4-(6-Hydroxy-2-(4-isopropylphenyl)-1-methyl-1,2,3,4-tetrahydroisoquinolin-1-yl)phenyl)acrylic Acid

1. Burks HE, et al. J Med Chem. 2017 Apr 13;60(7):2790-2818.

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