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Elacestrant
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Elacestrant图片
CAS NO:722533-56-4
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议

产品名称
依拉司群
RAD1901
产品介绍
Elacestrant 是一种具有口服活性的、选择性的雌激素受体 (ER) 降解剂 (SERD),能够作用于 ERα (IC50:48 nM)和 ERβ (IC50:870 nM)。

产品描述

Elacestrant with IC50s of 48 and 870 nM for ERα and ERβ, respectively.Elacestrant is an orally available selective estrogen receptor degrader .

体外活性

RAD1901 treatment exhibits dose-dependent inhibition of ERα expression, with an EC50 of 0.6 nM.?Treatment of ER-positive MCF-7 cells with E2 results in a potent and dose-dependent increase in proliferation, with an EC50 of 4 pM.?Treatment of cells with RAD1901 in the presence of 10 pM E2 resultsin a dose-dependent decrease in proliferation, with an IC50 value of 4.2 nM.RAD1901 selectively binds to and degrades the ER and is a potent antagonist of ER-positive breast cancer cell proliferation.?

体内活性

RAD1901 produces a robust and profound inhibition of tumor growth in MCF-7 xenograft models.?RAD1901 preserves ovariectomy-induced bone loss and preventes the uterotropic effects of E2.RAD1901-treated animals survived longer than those treated with either control or fulvestrant.?

Cas No.

722533-56-4

分子式

C30H38N2O2

分子量

458.63

别名

依拉司群;RAD1901

储存和溶解度

DMSO:60 mg/ml (130.82 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years