化学名称 : PHA-680632 /PHA680632
CAS : 398493-79-3
英文名称: PHA-680632
英文同义词: N-(2,6-Diethylphenyl)-4,6-dihydro-3-[[4-(4-methyl-1-piperazinyl)benzoyl]amino]pyrrolo[3,4-c]pyrazole-5(1h)-carboxamide
同义词: N-(2,6-二乙基苯基)-4,6-二氢-3-[[4-(4-甲基-1-哌嗪基)苯甲酰基]氨基]吡咯并[3,4-c]吡唑-5(1H)-甲酰胺
溶解度:DMSO
储存条件:-20C 2 years
生物活性
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.
参考文献
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