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

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.

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Phthalazinone pyrazole Chemical Structure

Phthalazinone pyrazole Chemical Structure

CAS No. : 880487-62-7

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Based on 1 publication(s) in Google Scholar

Phthalazinone pyrazole Related Antibodies

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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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Phthalazinone pyrazole Related Antibodies

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.
Appearance

Solid

Color

Brown to gray

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)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 11.11 mg/mL (35.01 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1512 mL 15.7560 mL 31.5119 mL
5 mM 0.6302 mL 3.1512 mL 6.3024 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1512 mL 15.7560 mL 31.5119 mL 78.7799 mL
5 mM 0.6302 mL 3.1512 mL 6.3024 mL 15.7560 mL
10 mM 0.3151 mL 1.5756 mL 3.1512 mL 7.8780 mL
15 mM 0.2101 mL 1.0504 mL 2.1008 mL 5.2520 mL
20 mM 0.1576 mL 0.7878 mL 1.5756 mL 3.9390 mL
25 mM 0.1260 mL 0.6302 mL 1.2605 mL 3.1512 mL
30 mM 0.1050 mL 0.5252 mL 1.0504 mL 2.6260 mL
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Phthalazinone pyrazole Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Phthalazinone pyrazole880487-62-7Aurora KinaseApoptosisoralepithelial-mesenchymal transitionhepatocyte-like cellEMTHLCshuman embryonic stem cellsAurora-A kinaseapoptosistumor growthInhibitorinhibitorinhibit

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