2. Epigenetics Cell Cycle/DNA Damage Apoptosis
  3. Aurora Kinase Apoptosis
  4. Aurora A-IN-5

Aurora A-IN-5 是一种高效且高选择性的 Aurora A 抑制剂 (IC50 = 0.02 μM)，其对 Aurora A 的选择性比 Aurora B 高 362 倍。Aurora A-IN-5 的选择性源于其独特的 C−H/π 相互作用、增强的疏水接触、开放的结合口袋以及更紧密的蛋白质堆积。Aurora A-IN-5 可抑制 Aurora A 的自身磷酸化，从而通过诱导 G2/M 期阻滞、触发细胞凋亡 (apoptosis) 和抑制克隆形成来抑制癌细胞增殖。Aurora A-IN-5 可抑制 MDA-MB-231 异种移植小鼠模型中的肿瘤生长。Aurora A-IN-5 可用于乳腺癌、宫颈癌、前列腺癌和淋巴瘤的相关研究。

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Aurora A-IN-5

Aurora A-IN-5 Chemical Structure

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Aurora A-IN-5 相关抗体

Top Publications Citing Use of Products

查看 Aurora Kinase 亚型特异性产品:

查看所有亚型
Aurora Kinase Aurora A Aurora B Aurora C

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Aurora A-IN-5 is a potent and highly selective Aurora A inhibitor (IC50 = 0.02 μM), showing 362-fold selectivity for over Aurora B. Aurora A-IN-5 shows its selectivity through unique C−H/π interactions, enhanced hydrophobic contacts, an open binding pocket, and tighter protein packing. Aurora A-IN-5 suppresses Aurora A autophosphorylation, thereby inhibiting cancer cell proliferation by inducing G2/M phase arrest, triggering apoptosis, and suppressing colony formation. Aurora A-IN-5 inhibits tumor growth in MDA-MB-231 xenograft mouse models. Aurora A-IN-5 can be used for breast, cervical, prostate, and lymphoma cancer research[1].

IC50 & Target[1]

Aurora A

0.02 μM (IC50)

体外研究
(In Vitro)

Aurora A-IN-5 (compound 5h) (48 小时) 对多种癌细胞系表现出强效的抗增殖活性，其 IC50 值分别为：K562 (2.87 μM)、MCF-7 (1.50 μM)、HeLa (0.85 μM)、DU145 (1.85 μM)、MOLT-4 (2.25 μM) 和 MDA-MB-231 (2.04 μM)[1]。
Aurora A-IN-5 (0.5 μM，48 小时) 可导致 MDA-MB-231 细胞纺锤体形态异常和染色体排列紊乱[1]。
Aurora A-IN-5 (2.5-10 μM，24 小时) 可通过阻滞 G2/M 期细胞周期进程，有效抑制 MDA-MB-231 细胞分裂[1]。
Aurora A-IN-5 (2-20 μM，24 小时) 以剂量依赖的方式诱导 MDA-MB-231 细胞凋亡[1]。
Aurora A-IN-5 (2 μM，14 天) 有效抑制 MDA-MB-231 细胞的克隆形成，从而抑制其增殖[1]。
Aurora A-IN-5 (0-1 μM) 对 Aurora A 在 Thr288 位点的磷酸化具有强效、选择性和剂量依赖性的抑制作用，同时，通过细胞热位移分析 (46-62 °C) 在 MDA-MB-231 细胞中显著稳定 Aurora A 蛋白，证实了其与靶点的直接结合[1]。
Aurora A-IN-5 对小鼠胚胎成骨细胞 MC3T3-E1 细胞表现出毒性 (IC50 = 7.135 μM)，但对正常肝脏 LO2 细胞表现出极小的毒性 (IC50 = 43.86 μM)[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Aurora A-IN-5 相关抗体:

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 2.0 μM
Incubation Time: 14 days
Result: Showed considerably fewer colonies (26 ± 3) compared to the untreated control group (106 ± 3).

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 2.0 and 20.0 μM
Incubation Time: 24 h
Result: Displayed a concentration-dependent increase in apoptotic cells, ranging from 11.5% at 2.0 μM to 88.6% at 20.0 μM.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 2.5, 5.0 and 10.0 μM
Incubation Time: 24 h
Result: Showed a significant ability to arrest MDA-MB-231 cells in the G2/M phase.
The percentage of cells in the G2/M phase gradually increased from 24.2% to 61.8% at 2.5 μM.

Immunofluorescence[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5 μM
Incubation Time: 48 h
Result: Displayed abnormal spindle configurations, either monopolar or multipolar, accompanied by various aberrations in chromosome alignment.
体内研究
(In Vivo)

Aurora A-IN-5 (30 mg/kg，腹腔注射，每两天一次，持续 20 天) 可抑制 MDA-MB-231 异种移植小鼠模型中的肿瘤生长[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c nude mice (1-5 weeks) subcutaneously injected with MDA-MB-231 cells[1]
Dosage: 30 mg/kg
Administration: i.p., every two days for 20 days
Result: Achieved a tumor growth inhibition rate of 73.0%.
Exhibited slightly increased body weight without any significant fluctuations throughout the treatment duration.
Revealed no significant parenchymal damage or inflammatory cell infiltration in vital organs such as the heart, liver, spleen, lung, and kidney.
分子量

459.54

Formula

C25H29N7O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Aurora A-IN-5 相关分类

  • 摩尔计算器

  • 稀释计算器

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Aurora A-IN-5Aurora KinaseApoptosisAurora AautophosphorylationMDA-MB-231xenograft modelsbreastcervicalprostatelymphomaK562HelaMCF-7DU145MOLT-4Inhibitorinhibitorinhibit

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