| 货号 | 16643-1mg |
| 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.1 Mutations of B-Raf, particularly at Val600, are common in melanomas and melanocytic nevi.1 SB-590885 is a potent inhibitor of B-Raf (Kd = 0.3 nM).2 It less effectively inhibits c-Raf (Ki = 1.72 nM) and has little effect at 46 other kinases.2,3 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.3,4 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.4 SB-590885 has also been used to study the role of B-Raf in cerebral ischemia.5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Tronnier, M. and Mitteldorf, C. Treating advanced melanoma: Current insights and opportunities. Cancer Manag.Res. 6, 349-356 (2014). 2.Takle, A.K.,Bamford, M.J.B.,Davies, S., et al. The identification of potent and selective imidazole-based inhibitors of B-Raf kinase. Bioorganic & Medicinal Chemistry Letters 18(15), 4373-4376 (2008). 3.King, A.J.,Patrick, D.R.,Batorsky, R.S., et al. Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885. Cancer Research 66(23), 11100-11105 (2006). 4.Klein, R.M. and Higgins, P.J. A switch in RND3-RHOA signaling is critical for melanoma cell invasion following mutant-BRAF inhibition. Molecular Cancer 10, 2-8 (2011). 5.Ahnstedt, H.,Säveland, H.,Nilsson, O., et al. Human cerebrovascular contractile receptors are upregulated via a B-Raf/MEK/ERK-sensitive signaling pathway. BMC Neuroscience 12, 1-9 (2011). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 453.5 |
| 分子式 | C27H27N5O2 |
| CAS号 | 405554-55-4 |
| 稳定性 | ≥ 2 years |
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