MK-0457
货号：
13600-250mg 基本售价：
6286.0 元 规格：
250 mg
产品信息
概述| 货号 | 13600-250mg |
| 描述 | The Aurora kinases (A, B, and C) are a family of serine-threonine kinases that regulate various stages of mitotic function. With significant roles in cell cycle and cell division, Aurora kinase gene amplification and overexpression are linked to tumorigenesis.1 MK-0457 is a potent pan-Aurora kinase inhibitor but favors Aurora A (Ki = 0.6 nM) over Aurora B (Ki = 18 nM) or Aurora C (Ki = 4.6 nM).2 It shows selectivity against a panel of more than 190 different protein kinases.2 MK-0457 effectively inhibits proliferation of several different cell lines of clear cell renal carcinoma (IC50s = <10 µM) and blocks the growth of tumors in a rodent model of cancer (80 mg/kg), inhibiting histone H3 phosphorylation and increasing apoptosis.1 By depleting Aurora activity, MK-0457 disrupts bipolar spindle formation during mitosis, arresting cell cycle progression at the G2/M phase.1 |
| 别名 | Tozasertib;VX-680; |
性能| 供应商 | Cayman |
| 应用文献 |
1.Li, Y.,Zhang, Z.F.,Chen, J., et al. VX680/MK-0457, a potent and selective Aurora kinase inhibitor, targets both tumor and endothelial cells in clear cell renal cell carcinoma. American Journal of Translational Research 2(3), 296-308 (2010).
2.Pollard, J.R. and Mortimore, M. Discovery and development of Aurora kinase inhibitors as anticancer agents. Journal of Medicinal Chemistry 52(9), 2629-2651 (2009).
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| 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 | 464.6 |
| 分子式 | C23H28N8OS |
| CAS号 | 639089-54-6 |
| 稳定性 | ≥ 2 years |
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