Ralaniten triacetate|1637573-04-6|(EPI-506)-陌孚医药/Medlife

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Ralaniten triacetate (Synonyms: EPI-506)

目录号: PL02627

CAS No. :1637573-04-6

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中文名称	Ralaniten triacetate
英文名称	Ralaniten triacetate
英文别名	Ralaniten acetate;L10K286T2H;Ralaniten acetate (USAN);Ralaniten acetate [USAN];HGHVYYKTOXUQNT-CLJLJLNGSA-N;D11185;(S)-3-(4-(2-(4-((S)-2-acetoxy-3-chloropropoxy)phenyl)propan-2-yl)phenoxy)propane-1,2-diyl diacetate;1,2-Propanediol, 3-(4-(1-(4-((2S)-2-(acetyloxy)-3-chloropropoxy)phenyl)-1-methylethyl)phenoxy)-, 1,2-diacetate, (2S)-;Ralaniten triacetate
Cas No.	1637573-04-6
分子式	C₂₇H₃₃ClO₈
分子量	521.00
包装储存	Pure form -20°C 3 years；4°C 2 years

产品详情

Ralaniten triacetate (EPI-506) 是 Ralaniten 的前药，是一种首创的，具有口服活性的雄激素受体 (AR) N 端结构域 (NTD) 抑制剂。Ralaniten triacetate 对全长和与抗性相关的 AR 物种，包括 AR-v7 都有活性。

生物活性

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.

性状

Liquid

体外研究(In Vitro)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Pure form -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[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 a

溶解度数据	In Vitro: DMSO : 100 mg/mL (191.94 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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