Aurora A inhibitor 2

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Aurora A inhibitor 2 

Aurora A inhibitor 2 (Compound 16h) 是一个有效的 Aurora A kinase 抑制剂,其 IC50 值为21.94 nM。Aurora A inhibitor 2 诱导 MDA-MB-231 细胞 caspase 依赖性凋亡 (apoptosis)。

Aurora A inhibitor 2

Aurora A inhibitor 2 Chemical Structure

CAS No. : 2412144-74-0

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生物活性

Aurora A inhibitor 2 (Compound 16h) is a potent Aurora A kinase inhibitor with an IC50 of 21.94 nM. Aurora A inhibitor 2 induces caspase-dependent apoptosis in MDA-MB-231 cells[1].

IC50 & Target

Aurora A

21.94 nM (IC50)

Aurora B

273.18 nM (IC50)

体外研究
(In Vitro)

Aurora A inhibitor 2 (Compound 16h) (0-20 µM, 48 h) shows potent antiproliferative activity against various human cancer cells, and inhibits colony formation[1].
Aurora A inhibitor 2 (0-4 µM, 24 h) inhibits the expression of phosphorylation of Aurora A and Histone H3 in a dose-dependent manner, and induces G2/M cell cycle arrest [1].
Aurora A inhibitor 2 (0-4 µM, 48 h) induces obvious apoptosis in MDA-MB-231 cells in a concentration-dependent manner[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: Breast cancer MDA-MB231, prostate cancer PC3, and neuroblastoma SH-SY5Y cells
Concentration: 0-20 µM
Incubation Time: 48 h
Result: Displayed potent antiproliferative activity with IC50 values of 0.38 ± 0.08, 1.09 ± 0.24, and 0.77 ± 0.12 µM against MDA-MB-231, PC3, and SH-SY5Y cells.

Western Blot Analysis[1]

Cell Line: MDAMB-231
Concentration: 1, 2, and 4 µM
Incubation Time: 24 h
Result: A dose-dependent and significant reduction in the phosphorylation of Aurora A and Histone H3 was observed. Significantly increased the levels of cleaved caspase 3/9 and cleaved-PARP.

Cell Cycle Analysis[1]

Cell Line: MDAMB-231
Concentration: 1, 2, and 4 µM
Incubation Time: 24 h
Result: Dose-dependently increased the and population of cells in the G2/M phase.

Apoptosis Analysis[1]

Cell Line: MDAMB-231
Concentration: 1, 2, and 4 µM
Incubation Time: 48 h
Result: Induced obvious apoptosis in a concentration-dependent manner.

分子量

446.50

Formula

C24H26N6O3

CAS 号

2412144-74-0

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.

参考文献
  • [1]. Chengcheng Fan, et al. Design, synthesis, biological evaluation of 6-(2-amino-1H-benzo[d]imidazole-6-yl)quinazolin-4(3H)-one derivatives as novel anticancer agents with Aurora kinase inhibition. Eur J Med Chem. 2020 Mar 15;190:112108.

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