Chemical Structure : Varilutamide
CAS No.:
1351185-54-0
Varilutamide
(ONC1-13B)
Catalog No.: PC-27513Not For Human Use, Lab Use Only.
Varilutamide (ONC1-13B) is a potent, nonsteroidal antagonist of androgen receptor, inhibits DHT-induced PSA expression with Ki of 20 nM, fully inhibits androgen-dependent gene expression.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
Varilutamide (ONC1-13B) is a potent, nonsteroidal antagonist of androgen receptor (AR), inhibits DHT-induced PSA expression with Ki of 20 nM, fully inhibits androgen-dependent gene expression.
Varilutamide (ONC1-13B) is around 10-fold more efficiently than bicalutamide (Ki 190 nM).
Varilutamide (ONC1-13B) inhibits DHT-induced cell proliferation of LnCAP cells.
Varilutamide (ONC1-13B) can completely inhibit 6a-Fluotestosterone induced AR nuclear translocation.
Varilutamide (ONC1-13B) ONC1-0013B (20 and 50 mg/kg once daily) efficiently inhibits tumor growth in the xenograft model of prostate cancer.
Physicochemical Properties
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M.Wt
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492.45
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Formula
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C22H16F4N4O3S
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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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(R)-4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-4-oxo-2-thioxo-7-oxa-1,3-diazaspiro[4.4]nonan-1-yl)-2-fluoro-N-methylbenzamide
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References
1. Ivachtchenko AV, et al. J Cancer. 2014 Jan 21;5(2):133-42.
2. Ivachtchenko AV, et al. Eur J Med Chem. 2015 Jun 24;99:51-66.
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