4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
详情描述
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。
产品详情
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。
生物活性
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 IC 50 of 7.4 μM. Ralaniten can be used for the research of castration-resistant prostate cancer (CRPC).
性状
Solid
IC50 & Target[1][2]
IC50: 7.4 μM (AR-NTD)
体外研究(In Vitro)
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.Ralaniten (10-35 μM; 4 h) inhibits transactivation of the AR N-terminal domain (NTD) induced by forskolin in LNCaP cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
EPI-002 (100 mg/kg; p.o. twice daily for 28 days) inhibits the VCaP tumor growth in castrated mice. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: Male NOD-SCID mice bearing subcutan
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (253.24 mM; Need ultrasonic)配制储备液
[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.