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)
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Ralaniten
CAS number：1203490-23-6 molecular formula：C21H27ClO5
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| Chinese alias | 拉拉尼滕 | ||
| English alias | Ralaniten | Ralaniten (USAN/INN) | 1,2-Propanediol, 3-(4-(1-(4-((2S)-3-chloro-2-hydroxypropoxy)phenyl)-1-methylethyl)phenoxy)-, (2R)- | E74798 | D11184 | AKOS040749271 | RALANITEN [INN] | (R)-3-(4-(2-(4-((S)-3-chloro-2-hydroxypropoxy)phenyl)propan-2-yl)ph | ||
| CAS number | 1203490-23-6 | molecular formula | C21H27ClO5 |
| molecular weight | 394.9 g/mol | Exact mass | ≥99% |
| PSA | 79.200 Ų | logp | 3.300 |
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