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BAY 1024767

Chemical Structure : BAY 1024767

CAS No.: 1273068-71-5

BAY 1024767 (BAY1024767)

Catalog No.: PC-35003Not For Human Use, Lab Use Only.

BAY 1024767 (BAY1024767) is a higly potent antagonist of androgen receptor (AR) wild-type (IC50=46 nM) and mutant forms located in the AR ligand-binding domain (LBD).

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    Biological Activity

    BAY 1024767 (BAY1024767) is a higly potent antagonist of androgen receptor (AR) wild-type (IC50=46 nM) and mutant forms located in the AR ligand-binding domain (LBD).
    BAY 1024767 inhibits mutants L701H, E709Y, V715M, W741C, H874Y (IC50=31 nM), F876L, T877A, M895T and M895V (IC50=11 nM).
    BAY 1024767 promotes nuclear localization of AR wild-type and mutants in the absence of R1881 in COS-7 cells.
    BAY 1024767 demonstrates KuCaP-1 prostate cancer model which bears the W741C bicalutamide resistance mutation and in the syngeneic prostate cancer rat model Dunning R3327-G.

    Physicochemical Properties

    M.Wt 492.517
    Formula C23H23F3N4O3S
    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-(3-((6-(2-hydroxy-2-methylpropoxy)pyridin-3-yl)methyl)-4,4-dimethyl-5-oxo-2-thioxoimidazolidin-1-yl)-2-(trifluoromethyl)benzonitrile

    References

    1. Sugawara T, et al. Oncotarget. 2016 Feb 2;7(5):6015-28.

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