| 货号 | 15142-1mg |
| 描述 | The Raf kinases activate cellular pathways that lead to cell proliferation and can contribute to certain types of cancer.1,2 Mutations in the kinase B-Raf are involved in a wide range of cancers.3,4 In particular, the mutation B-RafV600E occurs in melanomas and thyroid cancer but is poorly targeted by many inhibitors of wild type B-Raf.5,6 PLX4720 is an orally-available, highly selective inhibitor of B-RafV600E(IC50 = 13 nM).6 It is less effective against wild type B-Raf (IC50 = 160 nM) as well as several other kinases.6 PLX4720 induces cell cycle arrest and apoptosis in cells and xenografts expressing the mutant of B-Raf.5,6,7 |
| 别名 | Raf Kinase Inhibitor V; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Lyons, J.F.,Wilhelm, S.,Hibner, B., et al. Discovery of a novel Raf kinase inhibitor. Endocrine-Related Cancer 8(3), 219-225 (2001). 2.Wang, X. and Kim, J. Conformation-specific effects of Raf kinase inhibitors. Journal of Medicinal Chemistry 55(17), 7332-7341 (2012). 3.Flaherty, K.T.,Puzanov, I.,Kim, K.B., et al. Inhibition of mutated, activated BRAF in metastatic melanoma. New England Journal of Medicine 363(9), 809-819 (2010). 4.Old, W.M.,Shabb, J.B.,Houel, S., et al. Functional proteomics identifies targets of phosphorylation by B-Raf signaling in melanoma. Molecular Cell 34(1), 115-131 (2009). 5.Nucera, C.,Porrello, A.,Antonello, Z.A., et al. B-RafV600E and thrombospondin-1 promote thyroid cancer progression. Proceedings of the National Academy of Sciences of the United States of America 107(23), 10649-10654 (2010). 6.Tsai, J.,Lee, J.T.,Wang, W., et al. Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proceedings of the National Academy of Sciences of the United States of America 105(8), 3041-3046 (2008). 7.Nucera, C.,Nehs, M.A.,Nagarkatti, S.S., et al. Targeting BRAFV600E with PLX4720 displays potent antimigratory and anti-invasive activity in preclinical models of human thyroid cancer. Oncologist 16(3), 296-309 (2011). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 413.8 |
| 分子式 | C17H14ClF2N3O3S |
| CAS号 | 918505-84-7 |
| 稳定性 | ≥ 2 years |
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