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Amcenestrant
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。
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CAS NO:2114339-57-8
包装与价格:
包装价格(元)
2 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
1 mL*10 mM(in DMSO)电议

产品名称
SAR439859
产品介绍
SAR439859 是一种有效的 ER 拮抗剂,具有 ER 降解活性,EC50为 0.2 nM。它是一种具有口服活性,非甾体和选择性雌激素受体降解剂 (SERD)。它可在 ER+乳腺癌中表现出强大的抗肿瘤功效和有限的交叉耐药性。

产品描述

SAR439859 is an orally active, nonsteroidal and selective degrader of estrogen receptor (SERD). SAR439859 is a potent antagonist of ER (with an EC50 of 0.2 nM for ERα degradation).

体外活性

in vivo SAR439859 induces strong antitumor activity against a variety of BC cell lines and patient-derived xenografts, including models that harbor ERα mutations[1].

体内活性

SAR439859(orally; 2.5-25 mg/kg; twice daily for 30 days) exhibits substantial tumor-growth inhibition and displays tumor regression at the dose of 25 mg/kg/BID[1]. It is noticed that T1/2 was variable across species (1.98 h in mouse, 4.13 h in rat and 9.80 h in dog)[1].

Cas No.

2114339-57-8

分子式

C31H30Cl2FNO3

分子量

554.48

别名

SAR439859

储存和溶解度

DMSO:125 mg/mL (225.44 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years