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Phthalazinone pyrazole

 
Catalog No.
C3823
Aurora A激酶抑制剂
组合的产品项目
规格价格库存 数量
1mg
¥ 650.00
现货
5mg
¥ 2,930.00
现货
10mg
¥ 5,200.00
现货

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A

背景

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.

化学属性

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt317.4
Cas No.880487-62-7
FormulaC18H15N5O
Solubilityinsoluble in EtOH; insoluble in H2O; ≥7.14 mg/mL in DMSO
Chemical Name4-[(5-methyl-1H-pyrazol-3-yl)amino]-2H-phenyl-1-phthalazinone
SDFDownload SDF
Canonical SMILESO=C1C2=C(C=CC=C2)C(NC3=NNC(C)=C3)=NN1C4=CC=CC=C4
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质量控制

化学结构

Phthalazinone pyrazole