AG-126|118409-62-4|(Tyrphostin AG126)-陌孚医药/Medlife

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AG-126 (Synonyms: Tyrphostin AG126)

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

[1]. Cuzzocrea S, et al. The tyrosine kinase inhibitor tyrphostin AG126 reduces the development of acute and chronic inflammation. Am J Pathol. 2000 Jul;157(1):145-58. [Information]

[2]. Garg TK, et al. Oxidative stress causes ERK phosphorylation and cell death in cultured retinal pigment epithelium: prevention of cell death by AG126 and 15-deoxy-delta 12, 14-PGJ2. BMC Ophthalmol. 2003 Mar 21;3:5. [Information]

[3]. Dugo L, et al. The tyrosine kinase inhibitor tyrphostin AG 126 reduces the multiple organ failure induced by zymosan in the rat. Intensive Care Med. 2002 Jun;28(6):775-88. [Information]

[4]. Bullard LE, et al. Role for extracellular signal-responsive kinase-1 and -2 in retinal angiogenesis. Invest Ophthalmol Vis Sci. 2003 Apr;44(4):1722-31. [Information]

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

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产品使用指南

Data Sheet

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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