AS-703026
货号：
11226-1mg 基本售价：
350.0 元 规格：
1 mg
产品信息
概述| 货号 | 11226-1mg |
| 描述 | The mitogen-activated protein kinases, MEK1 and 2, are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the Ras-Raf-MEK-ERK pathway and are often upregulated in a variety of cancer cell types.1 AS-703026 is an orally bioavailable small molecule that selectively binds to and inhibits MEK1/2, preventing the activation of downstream effector proteins and transcription factors. It potently inhibits growth and survival of human INA-6 multiple myeloma cells and cytokine-induced osteoclast differentiation with IC50 values of 10 and 18.2 nM, respectively.2 In mice bearing H929 MM xenograft tumors, 30 mg/kg AS-703026 reduced tumor growth significantly, which correlated with downregulated ERK1/2 activity, induced PARP cleavage, and decreased microvessels in vivo.2 At 10 μM, AS-703026 supressed proliferation and transformation of K-Ras mutated colorectal cancer cells resistant to EGFR antibody therapy.3 |
| 别名 | MSC1936369B;Pimasertib; |
性能| 供应商 | Cayman |
| 应用文献 |
1.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).
2.Kim, K.,Kong, S.Y.,Fulciniti, M., et al. Blockade of the MEK/ERK signalling cascade by AS703026, a novel selective MEK1/2 inhibitor, induces pleiotropic anti-myeloma activity in vitro and in vivo. British Journal of Haematology 149(4), 537-549 (2010).
3.Yoon, J.,Koo, K.H. and Choi, K.Y. MEK1/2 inhibitors AS703026 and AZD6244 may be potential therapies for KRAS mutated colorectal cancer that is resistant to EGFR monoclonal antibody therapy. Cancer Research 71, 445-453 (2011).
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| 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 | 431.2 |
| 分子式 | C15H15FIN3O3 |
| CAS号 | 1236699-92-5 |
| 稳定性 | ≥ 2 years |
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