ODM-201(also known as BAY-1841788)is a novel, nonsteroidal, orally active AR inhibitor that inhibits potently androgen binding to AR and androgen-induced nuclear translocation of AR in AR overexpressing cells.
ODM-201 has been studied in phase I and phase II clinical trials and has thus far been found to be effective and well-tolerated, with the most commonly reported side effects including fatigue, nausea,and diarrhea. No seizures have been observed. As of July 2015, ODM-201 is in phase III trials for CRPC.
ORM-15341 is the main active metabolite of ODM-201. It, similarly, is a full antagonist of the AR, with an affinity (Ki) of 8 nM and an IC50 of 38 nM.
仅供研究使用。 我们不向患者出售。
名称 | ODM-201(BAY-1841788) |
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Iupac 化学名称 | N-((R)-1-(3-(4-cyano-3-(trifluoromethyl)phenyl)-1H-pyrazol-1-yl)propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide |
同义词 | BAY-1841788;ODM-201;ODM201;ODM 201;BAY1841788;BAY 1841788 |
英文同义词 | BAY-1841788;ODM-201;ODM201;ODM 201;BAY1841788;BAY 1841788 |
分子式 | C19H19ClN6O2 |
分子量 | 398.85 |
Smile | O=C(C1=NNC(C(O)C)=C1)N[C@H](C)CN2N=C(C3=CC=C(C#N)C(C(F)(F)F)=C3)C=C2 |
InChiKey | IQDIATJYQZUJNO-JHJMLUEUSA-N |
InChi | InChI=1S/C20H19F3N6O2/c1-11(25-19(31)18-8-17(12(2)30)26-27-18)10-29-6-5-16(28-29)13-3-4-14(9-24)15(7-13)20(21,22)23/h3-8,11-12,30H,10H2,1-2H3,(H,25,31)(H,26,27)/t11-,12?/m1/s1 |
Cas号 | 1297538-32-9 |
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