Phthalazinone pyrazole |
| Katalog-Nr.GC13668 |
Phthalazinonpyrazol ist ein potenter, selektiver und oral aktiver Inhibitor der Aurora-A-Kinase mit einem IC50 von 0,031 μM. Phthalazinonpyrazol kann die Mitose stoppen und anschließend das Tumorwachstum durch Apoptose proliferierender Zellen hemmen. Phthalazinonpyrazol unterdrÜckt die epithelial-mesenchymale Transition (EMT) wÄhrend der Differenzierung von hepatozytenÄhnlichen Zellen (HLCs) aus humanen embryonalen Stammzellen.
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Cas No.: 880487-62-7
Sample solution is provided at 25 µL, 10mM.
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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.
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