货号 | 4239/50 |
别名 | 4-[1-(6-Quinolinylmethyl)-1H-1,2,3- |
供应商 | Tocris |
生物活性 | Highly selective, high affinity MET inhibitor (Ki = 6-7 nM against wild type c-Met). Displays >1000-fold selectivity for c-Met over a panel of 208 kinases. |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >98 % |
计算分子量 | 468.49 |
分子式 | C19H16N8O.CH |
可溶性/溶解性 | Soluble to 100 mM in DMSO |
参考文献 | Cuiet al (2012) Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for the treatment of cancer. J.Med.Chem. 55 8091. PMID: 22924734. Underineret al (2010) Discovery of small molecule c-Met inhibitors: evolution and profiles of clinical candidates. Anticancer Agents Med.Chem. 10 7. PMID: 20015007. Ederet al (2009) Novel therapeutic inhibitors of the c-Met signaling pathway in cancer. Clin.Cancer Res. 15 2207. PMID: 19318488. Timofeevskiet al (2009) Enzymatic characterization of c-Met receptor tyrosine kinase oncogenic mutants and kinetic studies with aminopyridine and triazolopyrazine inhibitors. Biochemistry 48 5339. PMID: 19459657. |