2​ Biological Activity MLN8237 (Alisertib) is a selective Aurora kinase A inhibitor with median IC50 of 61 nM. MLN8237 (Alisertib) is a second-generation, orally bioavailable, highly selective small molecule inhibitor of the Aurora A kinase (serine/threonine protein kinase) with potential antineoplastic activity. MLN8237 binds to and inhibits Aurora A kinase, which may result in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregation, and inhibition of cell proliferation. After treatment in eight multiple myeloma cell lines with MLN8237 (Alisertib) (0.0001 μM – 4 μM) for 48 h, the affect of Aurora A kinase inhibition and a marked effect on both viability and proliferation (0.01 μM) was examined. Tumor burden was significantly reduced and overall survival was significantly increased in animals treated with 30 mg/kg MLN8237 (Alisertib). [1][2] 3​ References: Initial Testing of the Aurora Kinase A Inhibitor MLN8237 by the Pediatric Preclinical Testing Program (PPTP) John M. Maris,Christopher L. Morton,et al. Pediatr Blood Cancer 2010;55:26–34 Drug-Resistant Aurora A Mutants for Ce Target Validation of the Small Molecule Kinase Inhibitors MLN8054 and MLN8237 Dominic A. Sloane , Michael Z. Trikic ,et al. ACS CHEMICAL BIOLOGY 2010;5：536－576 The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.