Darolutamide CAS NO.1297538-32-9

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ODM-201 is a potent and full antagonists for human AR (hAR) with IC50 values of 26 nM by transactivation assays in AR-HEK293 cells.
IC50 value: 26 nM (in AR-HEK293 cells)
Target: androgen receptor
in vitro: ODM-201 is a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies. In competitive AR binding assays, the inhibition constant (Ki) values of ODM-201 were 11 nM.
in vivo: ODM-201 inhibits tumor growth in a castration-resistant VCaP xenograft model in vivo. ODM-201 shows a significant antitumor activity with both doses, 50 mg/kg twice daily being more efficacious compared to castrated, untreated mice (p < 0.001).