• 产品描述： Phthalazinone pyrazole is a potent, selective, and orally active inhibitor of Aurora-A kinase with an IC50 of 0.031 μM. Phthalazinone pyrazole can arrests mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells. Phthalazinone pyrazole suppresses the epithelial-mesenchymal transition (EMT) during the differentiation of hepatocyte-like cells (HLCs) from human embryonic stem cells

• 靶点： Aurora-A:0.031 μM (IC50);AuroraKinase

• 体外研究：
  Phthalazinone pyrazole (1 and 10 μM; 30 hours) enhances the proliferative capacity of HLCs. Phthalazinone pyrazole (1, 10, and 100 μM; 5 days) enhances hepatic morphological changes in differentiated HLCs without cytotoxicity. Phthalazinone pyrazole (1 and 10 μM; 5 and 17 days) suppresses the EMT and induced maturation of HLCs through the inhibition of the AKT signaling pathway by the off target effect with concomitant upregulation of HNF4α rather than direct inhibition of Aurora-A. The result is confirmed by western blot and qPCR. Cell Proliferation Assay Cell Line: Hepatocyte-like cells (HLCs) Concentration: 1 and 10 μM Incubation Time: 30 hours Result: Enhanced the proliferative capacity of HLCs. Cell Cytotoxicity Assay Cell Line: ES-HLCs, iPS-HLCs, Huh7 cells Concentration: 1, 10, and 100 μM Incubation Time: 5 days Result: Showed no cytotoxic effects on HLCs. Western Blot Analysis Cell Line: HLCs Concentration: 1 and 10 μM Incubation Time: 5 and 17 days Result: Markedly inhibited the phosphorylation of AKT and activated GSK-3β, which in turn inhibited Snail expression and increased HNF4α. Phthalazinone pyrazole didn’t significantly reduce the phosphorylation of Aurora-A..

• 参考文献：
  1. Prime ME, et al. Phthalazinone pyrazoles as potent, selective, and orally bioavailable inhibitors of Aurora-A kinase. J Med Chem. 2011;54(1):312-319. 2. Choi YJ, et al. Phthalazinone Pyrazole Enhances the Hepatic Functions of Human Embryonic Stem Cell-Derived Hepatocyte-Like Cells via Suppression of the Epithelial-Mesenchymal Transition. Stem Cell Rev Rep. 2018;14(3):438-450.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.151 ml	15.756 ml	31.512 ml
  5 mM	0.63 ml	3.151 ml	6.302 ml
  10 mM	0.315 ml	1.576 ml	3.151 ml
  50 mM	0.063 ml	0.315 ml	0.63 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *