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AG-126
ERK1(p44)和ERK2(p42)抑制剂,AG126 是酪氨酸激酶抑制剂,可以阻止丝裂原活化蛋白激酶 p42MAPK (ERK2) 的激活。
目录号: PC11839 纯度: ≥98%
CAS No. :118409-62-4
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中文名称
AG-126
中文别名
酪氨酸磷酸化抑制剂126
英文名称
AG-126
英文别名
Propanedinitrile,2-[(3-hydroxy-4-nitrophenyl)methylene]-;2-[(3-hydroxy-4-nitrophenyl)methylidene]propanedinitrile;AG-126;AG 127;Tyrphostin AG 126;Tyrphostin AG127;AG 126;TYRPHOSTIN A10;Tyrphostin 126;RARECHEM AL BX 0673;[3-HYDROXY-4-NITROBENZYLIDENE]MALONONITRILE;ALPHA-CYANO-(3-HYDROXY-4-NITRO)CINNAMONITRILE;ag127;AG126
Cas No.
118409-62-4
分子式
C10H5N3O3
分子量
215.17
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
生物活性

AG126 is a tyrosine kinase inhibitor, can inhibit the phosphorylation of ERK1 and ERK2 at 25-50 μM. AG126 can be used in meiosis, mitosis, and postmitotic research.

性状

Solid

IC50 & Target[1][2]

ERK2

 

体外研究(In Vitro)

AG126 (10 μM; overnight) increases the viability of ARPE-19 cells.
AG126 at concentrations higher than 10 μM show toxic to ARPE-19 cells and can enhance H2O2 toxicity.
AG126 (0.1-100 μM) inhibits VEGF-induced proliferation of BRMECs.

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

Cell Viability Assay

Cell Line: ARPE-19 cells
Concentration: 10 μM
Incubation Time: Overnight
Result: Increased the viability of ARPE-19 cells to 35-72% compared to the control.

Cell Proliferation Assay

Cell Line: BRMECs
Concentration: 0.1-100 μM
Incubation Time:
Result: Inhibited VEGF-induced proliferation of BRMECs in a dose-dependent manner.
体内研究(In Vivo)

AG 126 (intraperitoneal injection; 1-10 mg/kg; 1 h and 6 h after Zymosan treatment) treatment attenuates the degree of multiple organ failure (MOF) associated with Zymosan-induced peritonitis in the rat.

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

Animal Model: Male Sprague-Dawley rats treated with Zymosan (500 mg/kg)
Dosage: 10 mg/kg, 3 mg/kg or 1 mg/kg
Administration: Intraperitoneal injection; 10, 3, or 1 mg/kg; 1 h and 6 h after Zymosan treatment
Result: Attenuated the peritoneal exudation and the migration of polymorphonuclear cells caused by Zymosan in a dose-dependent fashion.
Attenuated the lung, liver, and intestinal injury.
Reduced the production of peroxynitrite and of pro-inflammatory cytokines TNF-alpha and IL-1beta.
运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
溶解度数据
体外研究: 

DMSO : 100 mg/mL (464.75 mM; Need ultrasonic and warming)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.6475 mL 23.2374 mL 46.4749 mL
5 mM 0.9295 mL 4.6475 mL 9.2950 mL
10 mM 0.4647 mL 2.3237 mL 4.6475 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。-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。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (11.62 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (11.62 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
*
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。

The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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