Pexmetinib

Pexmetinib is a dual inhibitor of Tie2 and p38 MAPK (IC50s = 1, 26, and 35 nM for Tie2, p38alpha, and p38beta, respectively). It also inhibits Abl, ARG, FGFR, FLT1, FLT4, Fyn, HCK, LYN, and MINK (IC50s = 4, 10, 28, 47, 42, 41, 26, 25, and 26 nM, respectively). Pexmetinib (0.5 and 1 µM) reduces proliferation of KG-1 and KT-1 leukemic cells in vitro.Formal Name: N-[3-(1,1-dimethylethyl)-1-(4-methylphenyl)-1H-pyrazol-5-yl]-N'-[[5-fluoro-2-[[1-(2-hydroxyethyl)-1H-indazol-5-yl]oxy]phenyl]methyl]-urea. CAS Number: 945614-12-0. Synonyms: ARRY 614. Molecular Formula: C31H33FN6O3. Formula Weight: 556.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 30 mg/ml. lambdamax: 310 nm. SMILES: FC1=CC(CNC(NC2=CC(C(C)(C)C)=NN2C3=CC=C(C)C=C3)=O)=C(OC4=CC=C(N(CCO)N=C5)C5=C4)C=C1. InChi Code: InChI=1S/C31H33FN6O3/c1-20-5-8-24(9-6-20)38-29(17-28(36-38)31(2,3)4)35-30(40)33-18-22-15-23(32)7-12-27(22)41-25-10-11-26-21(16-25)19-34-37(26)13-14-39/h5-12,15-17,19,39H,13-14,18H2,1-4H3,(H2,33,35,40). InChi Key: LNMRSSIMGCDUTP-UHFFFAOYSA-N.