| 货号 | 11599-10mg |
| 描述 | MEK kinases are central components of diverse intracellular signaling pathways. MEK1 and MEK2 specifically act downstream of growth factor receptors and the proto-oncogenes Ras and Raf to activate ERK1 and ERK2, often leading to an increase in cell proliferation.1 AZD 6244 is a potent, highly selective inhibitor of MEK1 and MEK2 (IC50 = 14 and 530 nM, respectively).2,3,1 It weakly inhibits the EGF receptor (IC50 = 7.0 µM) and has no effect on a large panel of other kinases.2 AZD 6244 suppresses the growth of tumors displaying high levels of phosphorylated MEK1/2 or ERK1/2.3,1 In addition to suppressing growth, it induces apoptosis and differentiation within tumors.4 AZD 6244 has potential, alone or in combination therapy, for promoting tumor regression in various forms of cancer, including those involving mutations of the proto-oncogenes Ras and Raf.5,6 |
| 别名 | ARRY-142886;NSC 741O78;CL 1,040;Selumetinib; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Yeh, T.C.,Marsh, V.,Bernat, B.A., et al. Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase ½ inhibitor. Clinical Cancer Research 13(5), 1576-1583 (2007). 2.Davis, M.I.,Hunt, J.P.,Herrgard, S., et al. Comprehensive analysis of kinase inhibitor selectivity. Nat.Biotechnol. 29(11), 1046-1051 (2011). 3.Huynh, H.,Soo, K.C.,Chow, P.K.H., et al. Targeted inhibition of the extracellular signal-regulated kinase kinase pathway with AZD6244 (ARRY-142886) in the treatment of hepatocellular carcinoma. Molecular Cancer Therapeutics 6(1), 138-146 (2007). 4.Davies, B.R.,Logie, A.,McKay, J.S., et al. AZD6244 (ARRY-142886), a potent inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase ½ kinases: mechanism of action in vivo, pharmacokinetic/pharmacodynamic relationship, and potential for combination in preclinical models. Molecular Cancer Therapeutics 6(8), 2209-2219 (2007). 5.Corcoran, R.B.,Cheng, K.A.,Hata, A.N., et al. Synthetic lethal interaction of combined BCL-XL and MEK inhibition promotes tumor regressions in KRAS mutant cancer models. Cancer Cell 23(1), 121-128 (2013). 6.Robert, C.,Dummer, R.,Gutzmer, R., et al. Selumetinib plus dacarbazine versus placebo plus dacarbazine as first-line treatment for BRAF-mutant metastatic melanoma: A phase 2 double-blind randomised study. Lancet Oncol. 14(8), 733-740 (2013). | |
| 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 | 457.7 |
| 分子式 | C17H15BrClFN4O3 |
| CAS号 | 606143-52-6 |
| 稳定性 | ≥ 2 years |
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