CH5183284

CH5183284 is a potent, selective inhibitor of the kinase activity of fibroblast growth factor receptors (FGFRs) 1, 2, and 3 (IC50s = 9.3, 7.6, and 22 nM, respectively). It less potently inhibits FGFR4 and platelet-derived growth factor receptor beta (IC50s = 290 and 560 nM, respectively) and displays IC50 values greater than 1 µM for a diverse panel of tyrosine and serine/threonine kinases. CH5183284 is effective against FGFR2 containing the gatekeeper mutation V564F. Moreover, it inhibits the growth of cancer cells expressing FGFR genetic alterations both in vitro and in xenograft mouse models.Formal Name: [5-amino-1-(2-methyl-1H-benzimidazol-6-yl)-1H-pyrazol-4-yl]-1H-indol-2-yl-methanone. CAS Number: 1265229-25-1. Synonyms: Debio 1347. Molecular Formula: C20H16N6O. Formula Weight: 356.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMSO: 1 mg/ml, DMSO:PBS (pH 7.2) (1:6): 0.1 mg/ml, Ethanol: 1 mg/ml. lambdamax: 212, 342 nm. SMILES: NC1=C(C(C2=CC3=C(C=CC=C3)N2)=O)C=NN1C4=CC(NC(C)=N5)=C5C=C4. InChi Code: InChI=1S/C20H16N6O/c1-11-23-16-7-6-13(9-17(16)24-11)26-20(21)14(10-22-26)19(27)18-8-12-4-2-3-5-15(12)25-18/h2-10,25H,21H2,1H3,(H,23,24). InChi Key: BEMNJULZEQTDJY-UHFFFAOYSA-N.