產(chǎn)品屬性:
產(chǎn)品名稱 | Ralaniten |
規(guī)格 | 100 mg |
貨號(hào) | EY-01Y14998 |
Cas No.: 1203490-23-6
別名: N/A
化學(xué)名: N/A
分子式: C21H27ClO5
分子量: 394.89
溶解度: DMSO : 100 mg/mL (253.24 mM; Need ultrasonic)
儲(chǔ)存條件: 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
產(chǎn)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.
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