CAS NO: | 1203490-23-6 |
包装: | 100mg |
市场价: | 7200元 |
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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation 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. |