BMS-641988 is a potent, selective, nonsteroidal androgen receptor antagonist with Ki of 1.7 nM, MDA-MB-453 cell IC50 of 16 nM.
BMS-641988 displays high selectivity over the glucocorticoid and progesterone receptors.
BMS-641988 displayed 3-7-fold increased antagonist activity of AR transactivation compared with bicalutamide.
BMS-641988 strongly inhibits androgen-dependent growth of the ventral prostate and seminal vesicles in rats, and is efficacious in CWR-22-BMSLD1 tumors initially refractory to treatment with bicalutamide.
