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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Aldose Reductase-GTx-560
GTx-560

Chemical Structure : GTx-560

CAS No.: 1459214-46-0

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GTx-560 (GTx560)

货号: PC-27248Not For Human Use, Lab Use Only.

GTx-560 is a potent, specific small-molecule inhibitor of aldo keto reductase 1C3 (AKR1C3), inhibits AKR1C3-dependent conversion of A'dione to testosterone in purified enzyme assays with IC50 of 2-3 uM, and IC50 of 10-50 nM in cell-based system.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

GTx-560 is a potent, specific small-molecule inhibitor of aldo keto reductase 1C3 (AKR1C3), inhibits AKR1C3-dependent conversion of A'dione to testosterone in purified enzyme assays with IC50 of 2-3 uM, and IC50 of 10-50 nM in cell-based system.
GTx-560 selectively inhibits AKR1C3-dependent AR transactivation, but not the 17β-HSD3- and AKR1C1-dependent transactivation in HEK-293 cells.
GTx-560 (10 uM) inhibits AKR1C3-dependent A'dione- and R1881-induced PSA gene expression and A'dione-induced LNCaP-AKR1C3 cell growth.
GTx-560 (30 mg/kg/d s.c. for 2 weeks) inhibits prostate cancer xenograft growth in animals bearing LNCaP-AKR1C3 tumors.

物理化学性质&存储条件

分子量 291.23
分子式 C15H8F3NO2
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

4-(3,4,5-trifluorophenyl)isoquinoline-1,6-diol

参考文献

1. Yepuru M, et al. Clin Cancer Res. 2013 Oct 15;19(20):5613-25.

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