Phthalazinone pyrazole

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Phthalazinonepyrazol 是一种有效的、选择性的、口服生物可利用的 Aurora-A 激酶抑制剂。 Aurora-A 在多种肿瘤类型中过度表达并表现出致癌活性。

Phthalazinone pyrazole is potent, selective, and orally bioavailable inhibitor of Aurora-A kinase. Aurora-A is overexpressed in a variety of tumor types and displays oncogenic activity.

Phthalazinone pyrazole (1 and 10 μM; 30 hours) enhances the proliferative capacity of HLCs.Phthalazinone pyrazole (1, 10, and 100 μM; 5 days) enhances hepatic morphological changes in differentiated HLCs without cytotoxicity.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.Cell Proliferation Assay 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 Cell Line:ES-HLCs, iPS-HLCs, Huh7 cellsConcentration:1, 10, and 100 μM Incubation Time:5 days Result:Showed no cytotoxic effects on HLCs.Western Blot Analysis 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 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.

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Cell Cycle/DNA Damage

Aurora Kinase

Aurora A

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880487-62-7

317.34

C18H15N5O

>98% (HPLC)

DMSO:10 mM

CC1=CC(NC(C2=C3C=CC=C2)=NN(C4=CC=CC=C4)C3=O)=NN1

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(-20℃)

With Ice Pack

≥ 2 years