Information Darolutamide (ODM-201) Darolutamide (ODM-201, BAY-1841788) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with K i of 11 nM. Phase 3. Targets Androgen receptor 11 nM(Ki) In vitro In AR-HEK293 cells stably expressing full-length hAR, ODM-201 inhibits human AR (hAR) with IC50 of 26 nM. ODM-201 inhibits VCaP cell proliferation with IC50 of 230 nM, while has no effect on the viability of AR-negative cell lines tested, DU-145 prostate cancer cells and H1581 lung cancer cells. In vivo In mice bearing VCaP xenografts, ODM-201 (50\u2009mg/kg, p.o.) significantly inhibits castration-resistant prostate tumor growth. Cell Research(from reference) Cell lines:DU-145, H1581, and VCaP cells Concentrations:~10 μM Incubation Time:4 days
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Darolutamide
CAS number:1297538-32-9 molecular formula:C19H19ClN6O2
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| Chinese alias | - | ||
| English alias | example 56 [US9657003] | N-((S)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)-propan-2-yl)-3-(1-hydroxyethyl)-1H-pyrazole-5-carboxamide | N-((S)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)propan-2-yl)-3-(1-hydroxyethyl)-1H-pyrazole-5-carboxamide | N-( | ||
| CAS number | 1297538-32-9 | molecular formula | C19H19ClN6O2 |
| molecular weight | 398.85 g/mol | Exact mass | - |
| PSA | 120.000 Ų | logp | 3.034 |
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