货号	规格	价格	上海	北京	珠海	重庆	武汉
S88209-5mg买3赠1	98.20%	￥310.00 S88209-5mg ￥310.00 现货（买3赠1）	4 4	-	-	-	-
S88209-10mg买3赠1	98.20%	￥500.00 S88209-10mg ￥500.00 现货（买3赠1）	6 6	-	-	-	-
S88209-25mg买3赠1	98.20%	￥1000.00 S88209-25mg ￥1000.00 现货（买3赠1）	6 6	-	-	-	-
S88209-100mg	≥98%	￥2280.00 S88209-100mg ￥2280.00 2-3天	0 货期：2-3天	-	-	-	-

大包装询价收藏产品

加入购物车

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

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

质检证书(COA)

输入产品批号：

如何获取质检证书(COA)?

请输入货号和一个与之匹配的批号。
例如:
批号：JS298415 货号：S20001-25g
在货品标签上如何找到货号和批号?

摩尔浓度计算器

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

质量

浓度

体积

分子摩尔量

计算重置