Phthalazinone pyrazole

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Phthalazinone pyrazole 

Phthalazinone pyrazole 是一种有效的、选择性的、具有口服活性的 Aurora-A 激酶抑制剂，其 IC50 值为 0.031 μM。Phthalazinone pyrazole 可以阻止有丝分裂并随后通过增殖细胞的凋亡抑制肿瘤生长。Phthalazinone pyrazole 抑制人胚胎干细胞向肝细胞样细胞 (HLC) 分化过程中的上皮间质转化 (EMT)。

Phthalazinone pyrazole

Phthalazinone pyrazole Chemical Structure

CAS No. : 880487-62-7

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生物活性

Phthalazinone pyrazole is a potent, selective, and orally active inhibitor of Aurora-A kinase with an IC50 of 0.031 μM. Phthalazinone pyrazole can arrests mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells. Phthalazinone pyrazole suppresses the epithelial-mesenchymal transition (EMT) during the differentiation of hepatocyte-like cells (HLCs) from human embryonic stem cells[1][2].

IC50 & Target

Aurora-A

0.031 μM (IC50)

体外研究
(In Vitro)

Phthalazinone pyrazole (1 and 10 μM; 30 hours) enhances the proliferative capacity of HLCs[2].
Phthalazinone pyrazole (1, 10, and 100 μM; 5 days) enhances hepatic morphological changes in differentiated HLCs without cytotoxicity[2].
Phthalazinone pyrazole (1 and 10 μM; 5 and 17 days) suppresses the EMT and induced maturation of HLCs through the inhibition of the AKT signaling pathway by the off target effect with concomitant upregulation of HNF4α rather than direct inhibition of Aurora-A. The result is confirmed by western blot and qPCR[2].

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

Cell Proliferation Assay[2]

Cell Line: Hepatocyte-like cells (HLCs)
Concentration: 1 and 10 μM
Incubation Time: 30 hours
Result: Enhanced the proliferative capacity of HLCs.

Cell Cytotoxicity Assay[2]

Cell Line: ES-HLCs, iPS-HLCs, Huh7 cells
Concentration: 1, 10, and 100 μM
Incubation Time: 5 days
Result: Showed no cytotoxic effects on HLCs.

Western Blot Analysis[2]

Cell Line: HLCs
Concentration: 1 and 10 μM
Incubation Time: 5 and 17 days
Result: Markedly inhibited the phosphorylation of AKT and activated GSK-3β, which in turn inhibited Snail expression and increased HNF4α. Phthalazinone pyrazole didn’t significantly reduce the phosphorylation of Aurora-A.

RT-PCR[2]

Cell Line: HLCs
Concentration: 1 and 10 μM
Incubation Time: 5 and 17 days
Result: Markedly inhibited the phosphorylation of AKT mRNA and activated GSK-3β mRNA, which in turn inhibited Snail mRNA expression and increased HNF4α mRNA. Phthalazinone pyrazole didn’t significantly reduce the phosphorylation of Aurora-A mRNA.

分子量

317.34

Formula

C18H15N5O
CAS 号

880487-62-7
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]. Prime ME, et al. Phthalazinone pyrazoles as potent, selective, and orally bioavailable inhibitors of Aurora-A kinase. J Med Chem. 2011;54(1):312-319.

    [2]. Choi YJ, et al. Phthalazinone Pyrazole Enhances the Hepatic Functions of Human Embryonic Stem Cell-Derived Hepatocyte-Like Cells via Suppression of the Epithelial-Mesenchymal Transition. Stem Cell Rev Rep. 2018;14(3):438-450.

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