Chemical Name : PHA-680632
CAS : 398493-79-3
Synonyms: N-(2,6-Diethylphenyl)-4,6-dihydro-3-[[4-(4-methyl-1-piperazinyl)benzoyl]amino]pyrrolo[3,4-c]pyrazole-5(1h)-carboxamide
Solubility:DMSO
Storage:-20C 2 years
Biologieal
MLN8237 is a second-generation, orally bioavailable, highly selective small molecule inhibitor of the e Aurora A kinase (serine/threonine protein kinas) 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 (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 30mg/kg MLN8237.
Reference
1. Mengkun Zhang. Effect of Aurora A kinase inhibitor MLN8237 combined with rituximab on antitumor activity in preclinical B-cell non-Hodgkin's lymphoma models. 2009 ASCO Annual Meeting