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Phthalazinone pyrazole
目录号: PC10221 纯度: ≥98%
CAS No. :880487-62-7
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中文名称
Phthalazinone pyrazole
中文别名
二氮杂萘酮吡唑
英文名称
Phthalazinone pyrazole
英文别名
1(2H)-Phthalazinone, 4-[(5-methyl-1H-pyrazol-3-yl)amino]-2-phenyl-;Phthalazinone pyrazole
Cas No.
880487-62-7
分子式
C18H15N5O
分子量
317.34
包装储存

Sealed and stored at 4℃

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

生物活性

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.

性状

Solid

IC50 & Target[1][2]

Aurora-A

0.031 μM (IC50)

体外研究(In Vitro)

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.

RT-PCR

Cell Line: HLCs
Concentration: 1 and 10 μM
Incubation Time: 5 and 17 days
Result: Markedly inhibited the phosphorylation of AKT mRNA and activated GSK-3β mRNA, which in turn inhibited Snail mRNA expression and increased HNF4α mRNA. Phthalazinone pyrazole didn’t significantly reduce the phosphorylation of Aurora-A mRNA.
运输条件

Room temperature or refrigerated transportation.

储存方式

Sealed and stored at 4℃

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

参考文献
溶解度数据
体外研究: 

DMSO : ≥ 11.11 mg/mL (35.01 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1512 mL 15.7560 mL 31.5119 mL
5 mM 0.6302 mL 3.1512 mL 6.3024 mL
10 mM 0.3151 mL 1.5756 mL 3.1512 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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