BAY-2402234

BAY-2402234 is an inhibitor of dihydroorotate dehydrogenase (DHODH, IC50 = 1.2 nM). It induces upregulation of the cell differentiation marker CD11b in MOLM-13 and HEL acute myeloid leukemia (AML) cells (EC50s = 3.16 and 0.96 nM, respectively) and inhibits the proliferation of nine leukemia cell lines (IC50s = 0.08-8.2 nM). BAY-2402234 induces cell cycle arrest at the G2/M phase and apoptosis in TF-1 cells in a concentration-dependent manner. In vivo, BAY-2402234 (1.25, 2.5, and 5 mg/kg) reduces tumor volume in an MV4-11 mouse xenograft model. It also increases survival in patient-derived xenograft (PDX) mouse models of AML.Formal Name: N-(2-chloro-6-fluorophenyl)-4-[4-ethyl-4,5-dihydro-3-(hydroxymethyl)-5-oxo-1H-1,2,4-triazol-1-yl]-5-fluoro-2-[(1S)-2,2,2-trifluoro-1-methylethoxy]-benzamide. CAS Number: 2225819-06-5. Molecular Formula: C21H18ClF5N4O4. Formula Weight: 520.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS (pH 7.2) (1:3): 0.25 mg/ml. SMILES: O=C1N(C2=CC(O[C@@H](C)C(F)(F)F)=C(C=C2F)C(NC3=C(C=CC=C3F)Cl)=O)N=C(CO)N1CC. InChi Code: InChI=1S/C21H18ClF5N4O4/c1-3-30-17(9-32)29-31(20(30)34)15-8-16(35-10(2)21(25,26)27)11(7-14(15)24)19(33)28-18-12(22)5-4-6-13(18)23/h4-8,10,32H,3,9H2,1-2H3,(H,28,33)/t10-/m0/s1. InChi Key: KNVJMHHAXCPZHF-JTQLQIEISA-N.