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Phthalazinone pyrazole
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Phthalazinone pyrazole图片
CAS NO:880487-62-7
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
Phthalazinone pyrazole 是一种有效的、选择性的、具有口服活性的 Aurora-A 激酶抑制剂,IC50 为 0.031 μM。 Phthalazinone pyrazole 可以阻止有丝分裂并随后通过增殖细胞的凋亡抑制肿瘤生长。 Phthalazinone pyrazole 抑制人胚胎干细胞向肝细胞样细胞 (HLC) 分化过程中的上皮-间质转化 (EMT)。
Cas No.880487-62-7
化学名4-[(5-methyl-1H-pyrazol-3-yl)amino]-2H-phenyl-1-phthalazinone
Canonical SMILESO=C1C2=C(C=CC=C2)C(NC3=NNC(C)=C3)=NN1C4=CC=CC=C4
分子式C18H15N5O
分子量317.4
溶解度≤0.15mg/ml in DMSO;0.25mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.