Phthalazinone pyrazole
Phthalazinone pyrazole is potent, selective, and orally bioavailable inhibitor of Aurora-A kinase [1]. The Aurora protein kinase family consists of Aurora-A, -B and –C. The Aurora kinases are important group of enzymes involved in controlling several aspects of cell division in mammalian cells. Dysfunction of these kinases has been associated with a failure to maintain a stable chromosome content, a state that can contribute to tumourigenesis. Aurora-A is overexpressed in a variety of tumor types and displays oncogenic activity [2].
In vitro: Phthalazinone pyrazole potently inhibited the activity of Aurora A kinase with an IC50 of 31 nM. It showed no inhibitory effect on Aurora B kinase at doses up to 100 μM. Phthalazinone pyrazole inhibited the proliferation of HCT116, Colo205, and MCF-7 cells with IC50 values of 7.8, 2.9, and 1.6 μM, respectively [1].
References:
[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.
[2] Vader G, Lens S M A. The Aurora kinase family in cell division and cancer[J]. Biochimica et Biophysica Acta (BBA)-Reviews on Cancer, 2008, 1786(1): 60-72.
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 317.4 |
| Cas No. | 880487-62-7 |
| Formula | C18H15N5O |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥7.14 mg/mL in DMSO |
| Chemical Name | 4-[(5-methyl-1H-pyrazol-3-yl)amino]-2H-phenyl-1-phthalazinone |
| SDF | Download SDF |
| Canonical SMILES | O=C1C2=C(C=CC=C2)C(NC3=NNC(C)=C3)=NN1C4=CC=CC=C4 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Chemical structure
