1. Cell Cycle/DNA Damage
    Epigenetics
  2. Aurora Kinase
  3. Phthalazinone pyrazole

Phthalazinone pyrazole 

Cat. No.: HY-12564 Purity: ≥98.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

Phthalazinone pyrazole Chemical Structure

Phthalazinone pyrazole Chemical Structure

CAS No. : 880487-62-7

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Description

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)

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].

MCE 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.
Molecular Weight

317.34

Formula

C18H15N5O

CAS No.
SMILES

O=C1C2=CC=CC=C2C(NC3=NNC(C)=C3)=NN1C4=CC=CC=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

References
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Phthalazinone pyrazole
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