货号 | 10012431-1mg |
描述 | The mitogen-activated protein (MAP) kinase intracellular signaling pathways are involved in the regulation of various cellular functions.1 One of these pathways, the Raf/MEK/ERK pathway, plays a major role in the regulation of cellular growth, differentiation, and proliferation. The modulation of this cascade has been studied as a useful approach to treating proliferative disorders such as cancer.2,3 PD 184161 is a potent and selective inhibitor of MEK1/2 with an IC50 value that ranges from 10-100 nM. 4 More effective at inhibiting phosphorylation of ERK1/2 than the selective MEK inhibitors, PD 098059 and U0126, PD 184161 is useful both in vitroandin vivo for studying the pharmacological role of the Raf/MEK/ERK pathway.4 PD 184161 is structurally related to clinically-studied MEK inhibitors PD184352 (CI-1040) and PD 325901 and has been shown to inhibit cell proliferation, induce apoptosis, and possess antitumor activity in MEK-dependent cancers.4 |
供应商 | Cayman |
应用文献 | |
1.Cowan, K.J. and Storey, K.B. Mitogen-activated protein kinases: New signaling pathways functioning in cellular responses to environmental stress. Journal of Experimental Biology 206, 1107-1115 (2003). 2.Dhillon, A.S.,Hagan, S.,Rath, S., et al. MAP kinase signalling pathways in cancer. Oncogene 26, 3279-3290 (2007). 3.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). 4.Klein, P.J.,Schmidt, C.M.,Wiesenauer, C.A., et al. The effects of a novel MEK inhibitor PD184161 on MEK-ERK signaling and growth in human liver cancer. Neoplasia 8(1), 1-8 (2006). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 557.6 |
分子式 | C17H13BrClF2IN2O2 |
CAS号 | 212631-67-9 |
稳定性 | ≥ 2 years |
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