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ORM-15341
本半岛bd体育手机客户端 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。
ORM-15341图片
CAS NO: 1297537-33-7
规格: 98%
分子量: 396.83
包装与价格:
包装 价格(元)
5mg 电议
10mg 电议
50mg 电议
100mg 电议

半岛bd体育手机客户端 介绍
ORM-15341是一种有效的雄激素受体(AR)拮抗剂,作用于AR-HEK293细胞,IC50值为38nM。
CAS:1297537-33-7
分子式:C19H17ClN6O2
分子量:396.83
纯度:98%
存储:Store at -20°C

Background:

ORM-15341 is a potent and full antagonist for human AR (hAR) with IC50 values of 38 nM as shown by transactivation assays in AR-HEK293 cells stably expressing full-length hAR and an androgen-responsive luciferase reporter gene construct.IC50 value: 38 nMTarget: androgen receptorin vitro: In competitive AR binding assays, the inhibition constant (Ki) values of ORM-15341 was 8 nM. ORM-15341 functions as a full antagonist for all tested mutant ARs , with IC50 of 25, 51, 700, and 1160 nM for wtAR, AR(F876L), AR(T877A), and AR(W741L).




[1]. Moilanen AM, et al. Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms toandrogen signaling-directed prostate cancer therapies. Sci Rep. 2015 Jul 3;5:12007. doi: 10.1038/srep12007. [2]. Toermaekangas Olli, et al. Preparation of heteroaryl carboxamides as androgen receptor modulators. From PCT Int. Appl. (2012), WO 2012143599 A1 20121026.


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