您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Ralaniten
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Ralaniten
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。
Ralaniten图片
包装:100mg
规格:98%
市场价:7056元
分子量:394.89

产品介绍
Ralaniten (EPI-002) 是一种有效和具有口服活性的雄激素受体 N 端结构域 (AR-NTD) 拮抗剂。Ralaniten 抑制 AR 转录活性,IC50 值为 7.4 μM。Ralanites 可用于去势抵抗性前列腺癌 (CRPC) 的研究。
货号:ajcx34210
CAS:1203490-23-6
分子式:C21H27ClO5
分子量:394.89
溶解度:DMSO : 100 mg/mL (253.24 mM; Need ultrasonic)
纯度:98%
存储:Store at -20°C
库存:现货

Background:

Ralaniten (EPI-002) is a potent and orally active antagonist of the androgen receptor-N-terminal domain (AR-NTD). Ralaniten inhibits AR transcriptional activity, with IC50 of 7.4 μM. Ralaniten can be used for the research of castration-resistant prostate cancer (CRPC)[1][2].

EPI-002 (5-35 μM; 2-3 days) reduces AR-dependent proliferation of LNCaP cells, and has no effect on the viability of PC3 human prostate cancer cells that do not express functional AR[1].Ralaniten (10-35 μM; 4 h) inhibits transactivation of the AR N-terminal domain (NTD) induced by forskolin in LNCaP cells[1].

EPI-002 (100 mg/kg; p.o. twice daily for 28 days) inhibits the VCaP tumor growth in castrated mice[1].

[1]. Myung JK, et, al. An androgen receptor N-terminal domain antagonist for treating prostate cancer. J Clin Invest. 2013 Jul;123(7):2948-60.
[2]. Yang YC, et, al. Targeting Androgen Receptor Activation Function-1 with EPI to Overcome Resistance Mechanisms in Castration-Resistant Prostate Cancer. Clin Cancer Res. 2016 Sep 1;22(17):4466-77.