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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
CAS NO:1203490-23-6
包装:100mg
市场价:7200元

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。
Cas No.1203490-23-6
别名EPI-002
分子式C21H27ClO5
分子量394.89
溶解度DMSO : 100 mg/mL (253.24 mM; Need ultrasonic)
储存条件4°C, protect from light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.