Ralaniten triacetate

产品说明书

Print
Chemical Structure| 1637573-04-6 同义名 : EPI-506
CAS号 : 1637573-04-6
货号 : A1275527
分子式 : C27H33ClO8
纯度 : 97%
分子量 : 520.999
MDL号 : N/A
存储条件:

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(201.54 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Ralaniten triacetate (EPI-506), a precursor of Ralaniten, is the first orally active inhibitor targeting the androgen receptor (AR) N-terminal domain (NTD). It is effective against both the full-length AR and variants associated with resistance, such as AR-v7[1][2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.92mL

0.38mL

0.19mL

9.60mL

1.92mL

0.96mL

19.19mL

3.84mL

1.92mL

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 after enzalutamide and/or abiraterone. Journal of Clinical Oncology 35 (2017): 5032-5032.