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Phthalazinone pyrazole
CAS No. 880487-62-7
Phthalazinone pyrazole( —— )
Catalog No. M24895 CAS No. 880487-62-7
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.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 258 | In Stock |
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| 10MG | 447 | In Stock |
|
| 25MG | 714 | In Stock |
|
| 50MG | 1017 | In Stock |
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| 100MG | 1368 | In Stock |
|
| 500MG | 2673 | In Stock |
|
| 1G | Get Quote | In Stock |
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Biological Information
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Product NamePhthalazinone pyrazole
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NoteResearch use only, not for human use.
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Brief DescriptionPhthalazinone 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.
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DescriptionPhthalazinone 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.
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In VitroPhthalazinone 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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In Vivo——
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Synonyms——
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PathwayCell Cycle/DNA Damage
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TargetAurora Kinase
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RecptorAurora A
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Research Area——
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Indication——
Chemical Information
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CAS Number880487-62-7
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Formula Weight317.34
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Molecular FormulaC18H15N5O
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Purity>98% (HPLC)
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SolubilityDMSO:10 mM
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SMILESCC1=CC(NC(C2=C3C=CC=C2)=NN(C4=CC=CC=C4)C3=O)=NN1
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Prime M E, Courtney S M, Brookfield F A, et al. Phthalazinone pyrazoles as potent, selective, and orally bioavailable inhibitors of Aurora-A kinase[J]. Journal of medicinal chemistry, 2010, 54(1): 312-319.
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