产品描述:
B-Raf is a MAP kinase kinase kinase, which functions downstream of Ras family GTPases to activate MEK1/2 and ERK1/2 signaling.{27148} Mutations of B-Raf, particularly at Val600, are common in melanomas and melanocytic nevi.{27148} SB-590885 is a potent inhibitor of B-Raf (Kd = 0.3 nM).{27151} It less effectively inhibits c-Raf (Ki = 1.72 nM) and has little effect at 46 other kinases.{27151,27149} SB-590885 blocks activation of ERK1/2 and anchorage-independent cell proliferation of melanoma cells with either wild type or V600E B-Raf at nanomolar concentrations.{27149,27150} Melanoma cells expressing the B-RafV600E mutation can drive invasion through alternative pathways in the presence of SB-590885, suggesting that combination therapy is needed to completely block cell invasion.{27150} SB-590885 has also been used to study the role of B-Raf in cerebral ischemia.{27152}