AZ 628

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 other types of cancer but is poorly targeted by many inhibitors of wild type B-Raf. AZ 628 is a quinazilinone that inhibits several Raf kinases, including B-Raf, B-RafV600E, and c-Raf-1 (IC50s = 105, 34, and 29 nM in in vitro kinase assays). It also prevents activation of several tyrosine kinases, including VEGFR2, DDR2, Lyn, Flt1, and FMS. In colon and melanoma cell lines carrying B-RafV600E mutations, AZ 628 is reported to inhibit anchorage-dependent and -independent growth, induce cell cycle arrest, and cause apoptosis.Formal Name: 3-(1-cyano-1-methylethyl)-N-[3-[(3,4-dihydro-3-methyl-4-oxo-6-quinazolinyl)amino]-4-methylphenyl]-benzamide. CAS Number: 878739-06-1. Molecular Formula: C27H25N5O2. Formula Weight: 451.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 0.25 mg/ml. lambdamax: 220, 225, 316 nm. SMILES: CC(C)(C#N)C1=CC=CC(C(NC2=CC(NC3=CC(C(N(C)C=N4)=O)=C4C=C3)=C(C)C=C2)=O)=C1. InChi Code: InChI=1S/C27H25N5O2/c1-17-8-9-21(31-25(33)18-6-5-7-19(12-18)27(2,3)15-28)14-24(17)30-20-10-11-23-22(13-20)26(34)32(4)16-29-23/h5-14,16,30H,1-4H3,(H,31,33). InChi Key: ZGBGPEDJXCYQPH-UHFFFAOYSA-N.