Chemical Structure : GTx-560
CAS No.:
1459214-46-0
GTx-560
(GTx560)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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291.23
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Formula
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C15H8F3NO2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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4-(3,4,5-trifluorophenyl)isoquinoline-1,6-diol
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References
1. Yepuru M, et al. Clin Cancer Res. 2013 Oct 15;19(20):5613-25.
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