Varilutamide (ONC1-13B)

Chemical Structure : Varilutamide

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货号: 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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100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	492.45
分子式	C22H16F4N4O3S
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	(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

参考文献

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.