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更新时间：2025-05-15 19:16:20浏览次数：219
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- 产品描述： Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity
- 靶点： Aurora A:1.2 nM (IC50);Aurora B:396.5 nM (IC50)
- 体内研究： Alisertib (MLN 8237) (30 mg/kg, p.o.) significantly reduces tumor burden and increases overall survival in xenograft-murine model of human-MM. Alisertib (3-30 mg/kg; p.o.; once daily for 3 weeks) causes tumor growth inhibition in solid tumor xenograft models.
- 参考文献：
1. Güllü G, et al. A novel Aurora-A kinase inhibitor MLN8237 induces cytotoxicity and cell-cycle arrest in multiple myeloma Blood June 24, 2010 vol. 115 no. 25 5202-5213. 2. Sloane DA, et al. Drug-Resistant Aurora A Mutants for Cellular Target Validation of the Small Molecule Kinase Inhibitors MLN8054 and MLN8237 ACS Chem. Biol., 2010, 5 (6), pp 563-576. 3. Bavetsias V, et al. Aurora Kinase Inhibitors: Current Status and Outlook. Front Oncol. 2015 Dec 21;5:278. 4. Manfredi MG, et al. Characterization of Alisertib (MLN8237), an investigational small-molecule inhibitor of aurora A kinase using novel in vivo pharmacodynamic assays.Clin Cancer Res. 2011 Dec 15;17(24):7614-7624.
- 溶解度： DMSO : 25 mg/mL (48.18 mM; Need ultrasonic)
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 1.927 ml 9.635 ml 19.27 ml 5 mM 0.385 ml 1.927 ml 3.854 ml 10 mM 0.193 ml 0.964 ml 1.927 ml 50 mM 0.039 ml 0.193 ml 0.385 ml
- 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的性，仅供客户参考交流研究之用。
