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ZM-447439

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Chemical Structure| 331771-20-1 同义名 : -
CAS号 : 331771-20-1
货号 : A107524
分子式 : C29H31N5O4
纯度 : 99%+
分子量 : 513.588
MDL号 : MFCD08703125
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(48.68 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Aurora A

    Aurora A, IC50:110 nM

  • Aurora B

    Aurora B, IC50:130 nM
描述 Cells treated with ZM-447439 enter interphase, proceed normally into mitosis, and assemble bipolar spindles. However, chromosome alignment, segregation, and cytokinesis all fail. ZM-447439 inhibits cell division and the mitotic phosphorylation of histone H3. It prevents chromosome alignment and separation, impairs spindle checkpoint function, and inhibits the kinetochore localization of BubR1, Mad2, and Cenp-E[1]. The inhibition of Aurora kinases by ZM-447439 reduces the phosphorylation of Ser10 on histone H3 in Hep2 cancer cells. Cells treated with ZM-447439 that are arrested in G2/M phase induce multipolar spindles and accumulate 4N/8N DNA, similar to cells with genetic suppression of Aurora-B. Treatment with ZM-447439 can induce apoptosis. The inhibition of Aurora kinases by ZM-447439 is closely associated with a reduction in the phosphorylation of Akt Ser473 and its substrates GSK3α/β Ser21 and Ser9[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
human A172 cell Growth inhibition assay Inhibition of human A172 cell growth in a cell viability assay, IC50=0.98411 μM SANGER
human A498 cell Growth inhibition assay Inhibition of human A498 cell growth in a cell viability assay, IC50=2.3669 μM SANGER
human ABC-1 cell Growth inhibition assay Inhibition of human ABC-1 cell growth in a cell viability assay, IC50=1.40352 μM SANGER
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.95mL

0.39mL

0.19mL

9.74mL

1.95mL

0.97mL

19.47mL

3.89mL

1.95mL
参考文献

[1]Ditchfield C, et al. Aurora B couples chromosome alignment with anaphase by targeting BubR1, Mad2, and Cenp-E to kinetochores. J Cell Biol. 2003 Apr 28;161(2):267-80.

[2]Long ZJ, et al. ZM 447439 inhibition of aurora kinase induces Hep2 cancer cell apoptosis in three-dimensionalculture. Cell Cycle. 2008 May 15;7(10):1473-9.