PLX4720

The Raf kinases activate cellular pathways that lead to cell proliferation and can contribute to certain types of cancer. Mutations in the kinase B-Raf are involved in a wide range of cancers. In particular, the mutation B-RafV600E occurs in melanomas and thyroid cancer but is poorly targeted by many inhibitors of wild type B-Raf. PLX4720 is an orally-available, highly selective inhibitor of B-RafV600E (IC50 = 13 nM). It is less effective against wild type B-Raf (IC50 = 160 nM) as well as several other kinases. PLX4720 induces cell cycle arrest and apoptosis in cells and xenografts expressing the mutant of B-Raf.Formal Name: N-[3-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide. CAS Number: 918505-84-7. Synonyms: Raf Kinase Inhibitor V. Molecular Formula: C17H14ClF2N3O3S. Formula Weight: 413.8. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:6): 0.1 mg/ml, Ethanol: 2 mg/ml. lambdamax: 214, 277 nm. SMILES: O=C(C1=C(F)C(NS(CCC)(=O)=O)=CC=C1F)C2=CNC3=NC=C(Cl)C=C32. InChi Code: InChI=1S/C17H14ClF2N3O3S/c1-2-5-27(25,26)23-13-4-3-12(19)14(15(13)20)16(24)11-8-22-17-10(11)6-9(18)7-21-17/h3-4,6-8,23H,2,5H2,1H3,(H,21,22). InChi Key: YZDJQTHVDDOVHR-UHFFFAOYSA-N.