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Proxalutamide

Chemical Structure : Proxalutamide

CAS No.: 1398046-21-3

Proxalutamide (GT-0918, GT0918)

Catalog No.: PC-70129Not For Human Use, Lab Use Only.

Proxalutamide (GT-0918) is a potent androgen receptor (AR) antagonist with ability to down regulate AR protein level in prostate cancer cells.

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    Biological Activity

    Proxalutamide (GT-0918) is a potent androgen receptor (AR) antagonist with ability to down regulate AR protein level in prostate cancer cells.
    Proxalutamide (GT-0918) is more potently inhibits androgen binding with AR's ligand binding domain than Bicalutamide (11.4-fold) and MDV3100 (3.5-fold) in biochemical assay.
    Proxalutamide (GT-0918) demonstrates stronger potency to block AR function of gene transcription in CRPC cells.
    Proxalutamide (GT-0918) demonstrates good anti-tumor efficacy among hormone sensitive, CRPC and AR+ breast cancer animal models.

    Physicochemical Properties

    M.Wt 517.5
    Formula C24H19F4N5O2S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    4-[4,4-Dimethyl-3-[6-[3-(2-oxazolyl)propyl]-3-pyridinyl]-5-oxo-2-thioxo-1-imidazolidinyl]-3-fluoro-2-(trifluoromethyl)benzonitrile

    References

    1. Youzhi Tong, et al. DOI: 10.1158/1538-7445.AM2014-614 Published October 2014

    2. Yang M, et al. Int J Pharm. 2014 Nov 20;475(1-2):97-109.

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