Phthalazinone pyrazole

Potent, selective inhibitor of Aurora kinase A

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库存: 现货

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1mg

￥962.00

770.00

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5mg

￥4262.00

3410.00

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10mg

￥7325.00

5860.00

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货号: ajci11578
CAS: 880487-62-7
别名:
分子式: C18H15N5O
分子量: 317.4
纯度: >98%
溶解度: ≤0.15mg/ml in DMSO;0.25mg/ml in dimethyl formamide
储存: Store at -20°C
库存: 现货

Background

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].

参考文献:
[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.