| 货号 | 16292-1mg |
| 描述 | The dual specificity mitogen-activated protein kinase kinases (MEK) isoforms MEK1 and MEK2 function in a RAS/RAF/MEK/ERK signaling pathway to control cell growth, survival, and differentiation. Trametinib is a potent inhibitor of both MEK 1 and 2 that works in an ATP-noncompetitive fashion (IC50s = 0.7 and 0.9 nM, respectively).1 It shows specificity for MEK1/2 over a panel of more than 180 kinases, including B-Raf, c-Raf, and MEK5.1 Trametinib blocks dual phosphorylation of ERK1/2 and stops cell cycling in cancer cell lines, both in vitro and in multiple tumor models in mice.1 Trametinib, alone or in combination with other chemotherapeutic drugs, targets a subset of cancer cells that can be characterized by specific biomarkers, such as B-Raf, RAS, or CTNNB1 mutations.1,2,3,4 |
| 别名 | GSK1120212;JTP-74057; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Gilmartin, A.G.,Bleam, M.R.,Groy, A., et al. GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition. Clinical Cancer Research 17(5), 989-1000 (2011). 2.Jing, J.,Greshock, J.,Holbrook, J.D., et al. Comprehensive predictive biomarker analysis for MEK inhibitor GSK1120212. Molecular Cancer Therapeutics 11(3), 720-729 (2012). 3.Leung, E.Y.,Kim, J.E.,Askarian-Amiri, M., et al. Relationships between signaling pathway usage and sensitivity to a pathway inhibitor: Examination of trametinib responses in cultured breast cancer lines. PLoS One 9(8), 1-12 (2014). 4.Uitdehaag, J.C.M.,de Roos, J.A.D.M.,van Doornmalen, A.M., et al. Comparison of the cancer gene targeting and biochemical selectivities of all targeted kinase inhibitors approved for clinical use. PLoS One 9(3), 1-13 (2014). | |
| 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 | 615.4 |
| 分子式 | C26H23FIN5O4 |
| CAS号 | 871700-17-3 |
| 稳定性 | ≥ 2 years |
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