产品描述:
MEK kinases are central components of diverse intracellular signaling pathways. MEK1 and MEK2 specifically act downstream of growth factor receptors and the proto-oncogenes Ras and Raf to activate ERK1 and ERK2, often leading to an increase in cell proliferation.{24267} AZD 6244 is a potent, highly selective inhibitor of MEK1 and MEK2 (IC50 = 14 and 530 nM, respectively).{24156,24266,24267} It weakly inhibits the EGF receptor (IC50 = 7.0 µM) and has no effect on a large panel of other kinases.{24156} AZD 6244 suppresses the growth of tumors displaying high levels of phosphorylated MEK1/2 or ERK1/2.{24266,24267} In addition to suppressing growth, it induces apoptosis and differentiation within tumors.{24265} AZD 6244 has potential, alone or in combination therapy, for promoting tumor regression in various forms of cancer, including those involving mutations of the proto-oncogenes Ras and Raf.{24269,24268}