Phthalazinone pyrazole
Based on 1 Customer Validation
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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- Pureté: 98.0%
- CAS No.: 880487-62-7
- Formule: C18H15N5O
- Masse moléculaire:317.34
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Voir tous les produits spécifiques à Isoform Aurora Kinase
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Activité biologique
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Aurora-A 0.031 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COLO 205 | IC50 |
2.9 μM
Compound: 7
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Cytotoxicity against human COLO205 cells
Cytotoxicity against human COLO205 cells
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[PMID: 21128645] |
| HCT-116 | IC50 |
7.8 μM
Compound: 7
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Cytotoxicity against human HCT116 cells after 5 days by celltiter-glo assay
Cytotoxicity against human HCT116 cells after 5 days by celltiter-glo assay
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[PMID: 21128645] |
| MCF7 | IC50 |
1.6 μM
Compound: 7
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Cytotoxicity against human MCF7 cells
Cytotoxicity against human MCF7 cells
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[PMID: 21128645] |
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.
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Cell Line:Hepatocyte-like cells (HLCs)
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Concentration:1 and 10 μM
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Incubation Time:30 hours
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Result:Enhanced the proliferative capacity of HLCs.
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Cell Line:ES-HLCs, iPS-HLCs, Huh7 cells
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Concentration:1, 10, and 100 μM
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Incubation Time:5 days
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Result:Showed no cytotoxic effects on HLCs.
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Cell Line:HLCs
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Concentration:1 and 10 μM
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Incubation Time:5 and 17 days
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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.
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Cell Line:HLCs
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Concentration:1 and 10 μM
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Incubation Time:5 and 17 days
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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.
Chemical Information
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CAS No. 880487-62-7
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Appearance Solid
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Masse moléculaire 317.34
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Formule C18H15N5O
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Color Brown to gray
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SMILES
O=C1C2=CC=CC=C2C(NC3=NNC(C)=C3)=NN1C4=CC=CC=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[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. [Content Brief]
[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. [Content Brief]
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 |
Phthalazinone pyrazole Related Classifications
HY-12564 Related Classifications
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