| 货号 | 16997-1mg |
| 描述 | Refametinib is an allosteric, selective inhibitor of MEK1 and MEK2 (IC50s = 19 and 47 nM, respectively).1 It blocks phosphorylation of ERK1/2 across several human cancer cell lines differing in tissue origin and BRAF mutational status (EC50s = 2.5-16 nM), inhibiting cell cycling in cancer cells but not in primary cells.1 Refametinib is orally available and active in human tumor xenograft models.1 It has potential utility, particularly in combination therapy, in certain forms of cancer.2,3,4 |
| 别名 | BAY 86-9766;RDEA119; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Iverson, C.,Larson, G.,Lai, C., et al. RDEA119/BAY 869766: A potent, selective, allosteric inhibitor of MEK1/2 for the treatment of cancer. Cancer Research 69(17), 6839-6847 (2009). 2.Diep, C.H.,Munoz, R.M.,Choudhary, A., et al. Synergistic effect between erlotinib and MEK inhibitors in KRAS wild-type human pancreatic cancer cells. Clinical Cancer Research 17(9), 2744-2756 (2011). 3.Schmieder, R.,Puehler, F.,Neuhaus, R., et al. Allosteric MEK1/2 inhibitor refametinib (BAY 86-9766) in combination with sorafenib exhibits antitumor activity in preclinical murine and rat models of hepatocellular carcinoma. Neoplasia 15(10), 1161-1171 (2013). 4.Akinleye, A.,Furgan, M.,Mukhi, N., et al. MEK and the inhibitors: From bench to bedside. J.Hematol.Oncol. 6, 1-11 (2013). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 572.3 |
| 分子式 | C19H20F3IN2O5S |
| CAS号 | 923032-37-5 |
| 稳定性 | ≥ 2 years |
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