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) 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo EPI-002 (100 mg/kg; p.o. twice daily for 28 days) inhibits the VCaP tumor growth in castrated mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male NOD-SCID mice bearing subcutaneous tumors were castrated Dosage: 100 mg/kg Administration: P.o. twice daily for 28 days Result: Inhibited the growth of castration-resistant prostate cancer (CRPC) xenografts that express AR splice variants . Form:Solid IC50& Target:IC50: 7.4 μM (AR-NTD)