Darolutamide

Darolutamide

【产品别名】BAY-1841788, ODM-201

【CAS号】 1297538-32-9

【目录编号】 2H-29

【纯度】 99.7%

【分子式】 C19H19ClN6O2

【分子量】 398.85

【简介】 ODM-201是一种新型androgen receptor (AR)拮抗剂,能够阻断AR核转运,其Ki为f 11 nM

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Darolutamide 详细介绍

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. [1]

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).[1]



[1]. Moilanen AM, et al. Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms toandrogen signaling-directed prostate cancer therapies. Sci Rep. 2015 Jul 3;5:12007. doi: 10.1038/srep12007.

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