|
產品描述： 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 |
|
靶點：
Aurora A:1.2 nM (IC50);Aurora B:396.5 nM (IC50);Apoptosis;AuroraKinase;Autophagy |
體內研究：
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. |
參考文獻：
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. |
|
溶解性：
DMSO : 25 mg/mL (48.18 mM; Need ultrasonic) |
|
保存條件：
-20℃ |
配置溶液濃度參考：
|
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： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
北京