| 货号 | 11580-50mg |
| 描述 | The dual specific threonine/tyrosine kinase, map kinase kinase (MEK), is a key component of the RAS/RAF/MEK/ERK signaling pathway that is frequently activated in human tumors.1,2 CI-1040 is a benzhydroxamate compound that potently inhibits MEK in an in vitro mitogen-activated protein kinase cascade assay with an IC50 value of 2.3 nM (Kd = 74 nM when activated with adenosine triphosphate).3,4 It can suppress phosphorylation of ERK in mouse colon 26 tumors with an IC50 value of 35 nM and demonstrates in vivo activity with oral administration in a mouse tumor model.3 The second-generation MEK inhibitor PD 0325901 (Item No. 13034) is a structural derivative of CI-1040 that was developed for improved solubility.3 |
| 别名 | PD 184352; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Vojtek, A.B., and Der, C.J. Increasing complexity of the Ras signaling pathway. The Journal of Biological Chemisty 273, 19925-19928 (1998). 2.Dorsam, R.T., and Gutkind, J.S. G-protein-coupled receptors and cancer. Nature Reviews.Cancer 7, 79-94 (2007). 3.Barret, S.D.,Bridges, A.J.,Dudley, D.T., et al. The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901. Bioorganic & Medicinal Chemistry Letters 18, 6501-6504 (2008). 4.VanScyoc, W.S.,Holdgate, G.A.,Sullivan, J.E., et al. Enzyme kinetics and binding studies on inhibitors of MEK protein kinase. Biochemistry 47, 5017-5027 (2008). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 478.7 |
| 分子式 | C17H14ClF2IN2O2 |
| CAS号 | 212631-79-3 |
| 稳定性 | ≥ 2 years |
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