| 货号 | 15336-1mg |
| 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 other types of cancer but is poorly targeted by many inhibitors of wild type B-Raf.5,6 AZ 628 is a quinazilinone that inhibits several Raf kinases, including B-Raf, B-RafV600E, and c-Raf-1 (IC50s = 105, 34, and 29 nM in in vitro kinase assays).7,8 It also prevents activation of several tyrosine kinases, including VEGFR2, DDR2, Lyn, Flt1, and FMS.7 In colon and melanoma cell lines carrying B-RafV600E mutations, AZ 628 is reported to inhibit anchorage-dependent and -independent growth, induce cell cycle arrest, and cause apoptosis.7 |
| 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.Khazak, V.,Astsaturov, I.,Serebriiskii, I.G., et al. Selective Raf inhibition in cancer therapy. Expert Opin.Ther.Targets 11(12), 1587-1609 (2007). 8.Montagut, C.,Sharma, S.V.,Shioda, T., et al. Elevated CRAF as a potential mechanism of acquired resistance to BRAF inhibition in melanoma. Cancer Research 68(12), 4853-4861 (2008). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 451.5 |
| 分子式 | C27H25N5O2 |
| CAS号 | 878739-06-1 |
| 稳定性 | ≥ 2 years |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |