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ZM-447439

点击次数:220发布时间:2013/4/7 16:59:49

ZM-447439

更新日期:2022/8/19 17:45:40

所 在 地:美洲

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简单介绍:ZM-447439技术数据:分子量(MW): 513.59 化学式: C29H31N5O4 溶解度: DMSO 103mg/mL Water <1mg/mL Ethanol <1mg/mL 纯度: >99% 稳定性: at -20℃ 2 years CAS号: 331771-20-1

相关标签:ZM-447439 331771-20-1 

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ZM-447439              
                     
            
上海义森生物科技有限公司

技术数据:

分子量(MW): 513.59 ZM-447439 Chemical Structure
化学式:

C29H31N5O4

溶解度: DMSO 103mg/mL   Water <1mg/mL   Ethanol <1mg/mL
纯度: >99%
稳定性: at -20℃ 2 years
CAS号: 331771-20-1

生物活性

 

ZM-447439 is a potent and selective Aurora B kinase inhibitor with an IC50 of 50 nM, 1 μM and 250 nM for Aurora B, A and C, respectively. Other kinases such as Cdk1 and PLK1 are not inhibited (up to 10 mM). Cells treated with ZM-447439 progress through interphase, enter mitosis and assemble bipolar spindles but chromosome alignment, segregation and cytokinesis all fail. Mitotic Aurora kinases are essential for accurate chromosome segregation during cell division. Forced overexpression of Aurora kinase results in centrosome amplification and multipolar spindles, causing aneuploidy, a hallmark of cancer. ZM447439 does not interfere with other kinases when used up to 5 µM. ZM447439 dose-dependently inhibited proliferation of all three cell lines (BON, QGP-1 and MIP-101) with IC50 values in the nanomolar to low micromolar range. Moreover, aurora kinase inhibition by ZM447439 potently induced apoptosis, which was accompanied by DNA fragmentation and caspase 3 and 7 activation. [1][2][3]

 

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