398493-79-3

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PHA-680632 /PHA680632

398493-79-3

编号ABP000945 化学名称PHA-680632 /PHA680632 英文名称 PHA-680632 分子式C28H35N7O2 分子量501.6232 纯度 >99%

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

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