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ZM-447439 {[allProObj[0].p_purity_real_show]}

货号:A107524

ZM-447439 是一种强效、选择性的 Aurora 激酶抑制剂,能够与 Aurora 激酶的活性位点结合,将 Aurora 激酶锁定在非活性构象中,从而阻断其在细胞有丝分裂过程中的关键作用。ZM-447439 通过诱导细胞周期停滞和凋亡,在 Hep2癌细胞等多种癌症的三维培养模型中显示出显著的抗癌潜力。

ZM-447439 化学结构 CAS号:331771-20-1
ZM-447439 化学结构
CAS号:331771-20-1
ZM-447439 3D分子结构
CAS号:331771-20-1
ZM-447439 化学结构 CAS号:331771-20-1
ZM-447439 3D分子结构 CAS号:331771-20-1
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ZM-447439 纯度/质量文件 产品仅供科研

货号:A107524 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Aurora A Aurora B Aurora C 其他靶点 纯度
BI-847325 ++

Aurora A (Human), IC50: 25 nM

++++

Aurora B (Xenopus laevis), IC50: 3 nM

++

Aurora C (Human), IC50: 15 nM

99%+
CCT 137690 ++

Aurora A, IC50: 15 nM

++

Aurora B, IC50: 25 nM

++

Aurora C, IC50: 19 nM

99%+
MK-5108 ++++

Aurora A, IC50: 0.064 nM

99%+
KW-2449 +

Aurora A, IC50: 48 nM

FLT3 99%+
Tozasertib ++++

Aurora A, Ki app: 0.6 nM

++

Aurora B, Ki app: 18 nM

+++

Aurora C, Ki app: 4.6 nM

FLT3,Bcr-Abl 99%+
AT9283 ++++

Aurora A, IC50: ~3.0 nM

++++

Aurora B, IC50: ~3.0 nM

99%+
MLN8054 +++

Aurora A, IC50: 4 nM

+

Aurora B, IC50: 172 nM

99%+
ZM-447439 +

Aurora A, IC50: 110 nM

+

Aurora B, IC50: 130 nM

Src 99%+
TCS7010 ++++

Aurora A, IC50: 3.4 nM

99%+
TAK-901 ++

Aurora A-TPX2, IC50: 21 nM

++

Aurora B-INCENP, IC50: 15 nM

99%+
Danusertib +++

Aurora A, IC50: 13 nM

+

Aurora B, IC50: 79 nM

+

Aurora C, IC50: 61 nM

RET 99%+
MK-8745 ++++

Aurora A, IC50: 0.6 nM

99+%
PHA-680632 ++

Aurora A, IC50: 27 nM

+

Aurora B, IC50: 135 nM

+

Aurora C, IC50: 120 nM

FLT3 99%+
AMG 900 +++

Aurora A, IC50: 5 nM

+++

Aurora B, IC50: 4 nM

++++

Aurora C, IC50: 1 nM

99%+
Alisertib ++++

Aurora A, IC50: 1.2 nM

99%+
ENMD-2076 +++

Aurora A, IC50: 14 nM

+

Aurora B, IC50: 350 nM

FLT3,RET 98%
JNJ-7706621 +++

Aurora A, IC50: 11 nM

++

Aurora B, IC50: 15 nM

99%+
CYC-116 +++

Aurora A, Ki: 8 nM

+++

Aurora B, Ki: 9 nM

FLT3 99%+
Reversine +++

Aurora A, IC50: 12 nM

+++

Aurora B, IC50: 13 nM

++

Aurora C, IC50: 20 nM

98%
CCT129202 ++

Aurora A, IC50: 42 nM

+

Aurora B, IC50: 198 nM

+

Aurora C, IC50: 227 nM

98%
SNS-314 mesylate +++

Aurora A, IC50: 9 nM

++

Aurora B, IC50: 31 nM

++++

Aurora C, IC50: 3 nM

99%+
Barasertib-HQPA ++++

Aurora B, IC50: 0.37 nM

99%+
Hesperadin +

Aurora B (human), IC50: 250 nM

98%
GSK-1070916 ++++

Aurora B-INCENP, IC50: 3.5 nM

+++

Aurora C-INCENP, IC50: 6.5 nM

SIK,Tie-2 99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

ZM-447439 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].

ZM-447439 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
human BE-13 cell Growth inhibition assay Inhibition of human BE-13 cell growth in a cell viability assay, IC50=0.84418 μM SANGER

ZM-447439 动物研究

Dose Mice: 80 mg/kg[3] (i.p.)
Administration i.p.

ZM-447439 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.

ZM-447439 实验方案

计算器
存储液制备 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

ZM-447439 技术信息

CAS号331771-20-1
分子式C29H31N5O4
分子量 513.588
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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
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