Ralaniten triacetate (Synonyms: EPI-506) |
| カタログ番号GC62603 |
ララニテンのプロドラッグであるララニテン トリアセテート (EPI-506) は、クラス初の経口活性アンドロゲン受容体 (AR) N 末端ドメイン (NTD) 阻害剤です。ララニテン トリアセテートは、AR-v7 を含む全長および抵抗性関連の AR 種の両方に対して活性を示します。
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Cas No.: 1637573-04-6
Sample solution is provided at 25 µL, 10mM.
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Ralaniten triacetate (EPI-506), the pro-drug of Ralaniten, is a first-in-class, orally active androgen receptor (AR) N-terminal domain (NTD) inhibitor. Ralaniten triacetate shows activity against both full length and resistance-related AR species, including AR-v7[1][2].
Ralaniten triacetate (EPI-506) targets the N-terminal domain of the androgen receptor (AR), and is used for metastatic castration-resistant prostate cancer (mCRPC) research. EPI-506 is a first-in-class, highly-specific small molecule that binds to a novel target on the AR, the N-terminal domain (NTD) and directly inhibits AR transcriptional activity by blocking the interaction of the AR with transcriptional proteins[2].
[1]. Obst JK, et al. Revealing Metabolic Liabilities of Ralaniten To Enhance Novel Androgen Receptor Targeted Therapies. ACS Pharmacol Transl Sci. 2019;2(6):453-467. Published 2019 Sep 26.
[2]. Chi, Kim Nguyen et al. Efficacy, safety, tolerability, and pharmacokinetics of EPI-506 (ralaniten acetate), a novel androgen receptor (AR) N-terminal domain (NTD) inhibitor, in men with metastatic castration-resistant prostate cancer (mCRPC) progressing after enzalutamide and/or abiraterone. Journal of Clinical Oncology 35 (2017): 5032-5032.
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