Ralaniten (Synonyms: EPI-002) |
| カタログ番号GC62683 |
Ralaniten (EPI-002) は、アンドロゲン受容体 N 末端ドメイン (AR-NTD) の強力な経口活性アンタゴニストです。ララニテンは AR 転写活性を阻害し、IC50 は 7.4 μM です。 Ralaniten は、去勢抵抗性前立腺癌 (CRPC) の研究に使用できます。
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Cas No.: 1203490-23-6
Sample solution is provided at 25 µL, 10mM.
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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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