ODM-201

ODM-201 is an androgen receptor (AR) antagonist (Ki = 11 nM). It inhibits AR transactivation in U2OS osteosarcoma cells expressing human wild-type and mutant ARs (IC50s = 65, 66, 1,500, and 1,782 nM for wild-type, ARF876L, ARW741L, and ART877A, respectively). ODM-201 prevents androgen-induced AR nuclear translocation in AR-overexpressing HS-HEK293 and LNCaP cells and suppresses androgen-induced proliferation of VCaP cells (IC50 = 230 nM). In vivo, ODM-201 (50 mg/kg per day) reduces tumor growth in a VCaP castrated mouse xenograft model. It also inhibits tumor growth without increasing serum testosterone levels in a VCaP intact mouse xenograft model.Formal Name: N-[(1S)-2-[3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl]-1-methylethyl]-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide. CAS Number: 1297538-32-9. Synonyms: BAY 1841788. Molecular Formula: C19H19ClN6O2. Formula Weight: 398.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 25 mg/ml, DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml, Ethanol: 10 mg/ml. lambdamax: 288 nm. SMILES: OC(C)C1=CC(C(N[C@@H](C)CN2C=CC(C3=CC=C(C#N)C(Cl)=C3)=N2)=O)=NN1. InChi Code: InChI=1S/C19H19ClN6O2/c1-11(22-19(28)18-8-17(12(2)27)23-24-18)10-26-6-5-16(25-26)13-3-4-14(9-21)15(20)7-13/h3-8,11-12,27H,10H2,1-2H3,(H,22,28)(H,23,24)/t11-,12?/m0/s1. InChi Key: BLIJXOOIHRSQRB-PXYINDEMSA-N.