2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. Aurora Kinase Apoptosis
  4. Phthalazinone pyrazole

Phthalazinone pyrazole 

目录号: HY-12564 纯度: ≥98.0%
COA 产品使用指南

摩尔计算器

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，其 IC50 值为 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)。

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Phthalazinone pyrazole Chemical Structure

Phthalazinone pyrazole Chemical Structure

CAS No. : 880487-62-7

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Customer Review

Phthalazinone pyrazole 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1][2].

IC50 & Target

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[2].
Phthalazinone pyrazole (1, 10, and 100 μM; 5 days) enhances hepatic morphological changes in differentiated HLCs without cytotoxicity[2].
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[2].

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

Phthalazinone pyrazole 相关抗体:

Cell Proliferation Assay[2]

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[2]

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[2]

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[2]

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.
分子量

317.34

Formula

C18H15N5O
CAS 号
性状

固体

颜色

Brown to gray

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

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

溶解性数据
细胞实验： 

DMSO 中的溶解度 : ≥ 11.11 mg/mL (35.01 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
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
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

Phthalazinone pyrazole 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1512 mL 15.7560 mL 31.5119 mL 78.7799 mL
5 mM 0.6302 mL 3.1512 mL 6.3024 mL 15.7560 mL
10 mM 0.3151 mL 1.5756 mL 3.1512 mL 7.8780 mL
15 mM 0.2101 mL 1.0504 mL 2.1008 mL 5.2520 mL
20 mM 0.1576 mL 0.7878 mL 1.5756 mL 3.9390 mL
25 mM 0.1260 mL 0.6302 mL 1.2605 mL 3.1512 mL
30 mM 0.1050 mL 0.5252 mL 1.0504 mL 2.6260 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Phthalazinone pyrazole880487-62-7Aurora KinaseApoptosisoralepithelial-mesenchymal transitionhepatocyte-like cellEMTHLCshuman embryonic stem cellsAurora-A kinaseapoptosistumor growthInhibitorinhibitorinhibit

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