| Identification | Back Directory | [Name]
Alisertib sodium salt | [CAS]
1028486-06-7 | [Synonyms]
MLN 8237 sodium
Alisertib sodium salt
2H6]-Alisertib sodium salt | [Molecular Formula]
C27H21ClFN4NaO4 | [MOL File]
1028486-06-7.mol | [Molecular Weight]
542.93 |
| Hazard Information | Back Directory | [Uses]
Alisertib (MLN 8237) sodium 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 sodium induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity[1][2][3]. | [in vivo]
Alisertib (MLN 8237) (30 mg/kg, p.o.) significantly reduces tumor burden and increases overall survival in xenograft-murine model of human-MM[1].
Alisertib (3-30 mg/kg; P.o.; once daily for 3 weeks) causes tumor growth inhibition in solid tumor xenograft models[4]. | Animal Model: | Nude mice bearing HCT-116 colon tumor xenograft[4] | | Dosage: | 3, 10, or 30 mg/kg | | Administration: | P.o.; once daily for 3 weeks | | Result: | Resulted in a dose-dependent TGI (tumor growth inhibition) of 43.3%, 84.2%, and 94.7% for the 3, 10, and 30 mg/kg groups,respectively.
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| [IC 50]
Aurora A: 12.5 nM (IC50); Aurora B: 396.5 nM (IC50) | [References]
[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. DOI:10.1182/blood-2009-12-259523
[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. DOI:10.1021/cb100053q
[3] Bavetsias V, et al. Aurora Kinase Inhibitors: Current Status and Outlook. Front Oncol. 2015 Dec 21;5:278. DOI:10.3389/fonc.2015.00278
[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. DOI:10.1158/1078-0432.CCR-11-1536 |
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BOC Sciences
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1-631-485-4226; 16314854226 |
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https://www.bocsci.com |
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