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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Cytochrome P450 (CYPs)-Seviteronel
Seviteronel

Chemical Structure : Seviteronel

CAS No.: 1610537-15-9

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Seviteronel (VT-464, VT464)

货号: PC-25060Not For Human Use, Lab Use Only.

Seviteronel (VT-464) is a potent, selective and oral inhibitor of CYP17A1 inhibitor with 17,20-lyase IC50 of 69 nM, 10-fold selective over 17α-hydroxylase.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Seviteronel (VT-464) is a potent, selective and oral inhibitor of CYP17A1 inhibitor with 17,20-lyase IC50 of 69 nM, 10-fold selective over 17α-hydroxylase.
Seviteronel (VT-464) demonstrated a greater decrease in AR transactivation compared with abiraterone (ABI).
Seviteronel (VT-464) suppressed the AR axis to a greater extent compared with ABI.
Seviteronel (VT-464) reduced AR signaling more effectively than abiraterone in cultured PCa cells expressing T877A AR mutant.
Seviteronel (VT-464) reduced the increase in tumor volume in castrate male mice of CRPC patient-derived xenograft, MDA-PCa-133 expressing H874Y AR mutant.

物理化学性质&存储条件

分子量 399.35
分子式 C18H17F4N3O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(S)-1-(6,7-bis(difluoromethoxy)naphthalen-2-yl)-2-methyl-1-(1H-1,2,3-triazol-5-yl)propan-1-ol

参考文献

1. Rafferty SW, et al. Bioorg Med Chem Lett. 2014 Jun 1;24(11):2444-7.

2. Toren PJ, et al. Mol Cancer Ther. 2015 Jan;14(1):59-69.

3. Maity SN, et al. Sci Rep. 2016 Oct 17;6:35354. doi: 10.1038/srep35354.

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