货号 | 4836/50 |
别名 | 3-(1-Cyano-1-methylethyl)-N-[3-[(3, |
供应商 | Tocris |
生物活性 | Potent, ATP-competitive inhibitor of Raf kinases (IC50 values are 29, 34 and 105 nM for c-Raf1, B-RafV600E and wild-type B-Raf, respectively). Displays selectivity for Raf kinases over a panel of 150 other kinases; inhibits activation of tyrosine protein kinases such as VEGFR2, Lyn, Flt1 and Fms. Also inhibits growth, and induces cell cycle arrest and apoptosis in colon and melanoma cell lines with the B-RafV600Emutation. |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >98 % |
计算分子量 | 451.52 |
分子式 | C27H25N5O2 |
可溶性/溶解性 | Soluble to 100 mM in DMSO |
参考文献 | Hatzivassiliouet al (2010) RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth. Nature 464 431. PMID: 20130576. Montagutet al (2008) Elevated CRAF as a potential mechanism of acquired resistance to BRAF inhibition in melanoma. Cancer Res. 68 4853. PMID: 18559533. Khazaket al (2007) Selective Raf inhibition in cancer therapy. Expert Opin.Ther.Targets 11 1587. PMID: 18020980. |