2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. Aurora Kinase Apoptosis
  4. Aurora kinase-IN-8

Aurora kinase-IN-8 是一种有口服活性的 Aurora 激酶抑制剂。Aurora kinase-IN-8 对Aurora A 激酶和Aurora B 激酶的 IC50 值分别为 2.8 nM 和 28.1 nM。Aurora kinase-IN-8 能够阻止纺锤体形成、导致 G2/M 期阻滞并诱导细胞凋亡 (apoptosis)。Aurora kinase-IN-8 可用于癌症研究，如三阴性乳腺癌。

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Aurora kinase-IN-8

Aurora kinase-IN-8 Chemical Structure

CAS No. : 1911629-44-1

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Aurora kinase-IN-8 相关抗体

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查看 Aurora Kinase 亚型特异性产品:

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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 kinase-IN-8 is a orally active Aurora kinase inhibitor. Aurora kinase-IN-8 shows IC50 values of 2.8 and 28.1 nM against Aurora A kinase and Aurora B kinase. Aurora kinase-IN-8 can prevent spindle formation, cause G2/M phase arrest, and induce cell apoptosis. Aurora kinase-IN-8 can be used for the research of cancer, such as triple-negative breast cancer[1].

IC50 & Target[1]

Aurora A

2.8 nM (IC50)

Aurora B

28.1 nM (IC50)

体外研究
(In Vitro)

Aurora kinase-IN-8 (Compound 9h) 对 MDA-MB-231 细胞表现出优异的活性，其 IC50 值为 48 nM，对其他癌细胞的 IC50 值范围为 40-560 nM[1]。
Aurora kinase-IN-8 (1 μM, 48 h) 可抑制 MDA-MB-231 细胞中 Aurora A 激酶的磷酸化[1]。
Aurora kinase-IN-8 (1 μM, 48 h) 可抑制 MDA-MB-231 细胞中的纺锤体形成[1]。
Aurora kinase-IN-8 (0.3-1.2 μM, 24 h) 可诱导 MDA-MB-231 细胞发生 G2/M 期阻滞和凋亡[1]。

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

Aurora kinase-IN-8 相关抗体:

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 1 μM
Incubation Time: 48 h
Result: Inhibited Aurora A kinase phosphorylation.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.3 and 0.6 μM
Incubation Time: 24 h
Result: Caused cell cycle G2/M phase arrest and aneuploidy.
体内研究
(In Vivo)

Aurora kinase-IN-8 (Compound 9h) (30 mg/kg，灌胃给药，每 2 天一次，持续 19 天) 在 MDA-MB-231 异种移植肿瘤小鼠模型中显著抑制肿瘤生长[1]。

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

Animal Model: MDA-MB-231 xenograft tumor mice models[1]
Dosage: 30 mg/kg
Administration: Orally gavage, every 2 days for 19 days
Result: Showed a tumor growth inhibition (TGI) rate of 59%.
Reduced tumor weight and volume.
Had no significant impact on mouse body weight and liver/lung weight.
分子量

425.53

Formula

C25H27N7
CAS 号
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 kinase-IN-8 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Aurora kinase-IN-81911629-44-1Aurora KinaseApoptosisAurora kinaseAurora A kinaseAurora B kinaseTriple-negative breast cancerMDA-MB-231Inhibitorinhibitorinhibit

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