878739-06-1 in bulk supply 878739-06-1 in stock AZ-628 good supplier CAS NO.878739-06-1

878739-06-1 in bulk supply 878739-06-1 in stock AZ-628 good supplier

AZ 628 is a potent, ATP-competitive inhibitor of Raf kinases (IC₅₀ values are 29, 34 and 105 nM for c-Raf1, B-Raf^V600E and wild-type B-Raf, respectively). Displays selectivity for Raf kinases over a panel of 150 other kinases; inhibits activation of tyrosine protein kinases such as VEGFR2, Lyn, Flt1 and Fms. Also inhibits growth, and induces cell cycle arrest and apoptosis in colon and melanoma cell lines with the B-Raf^V600E mutation.

AZ628 is a potent tyrosine protein inhibitor to wild-type Raf-1 and Raf-B V600E with IC50 of 29 nM and 34 nM, respectively.

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-Raf^V600E 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-Raf^V600E, 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-Raf^V600E mutations, AZ 628 is reported to inhibit anchorage-dependent and -independent growth, induce cell cycle arrest, and cause apoptosis.