您好，欢迎来到试剂仪器网！ [登录] [免费注册]
试剂仪器网
发布求购
位置：首页 > 产品库 > AG 556
立即咨询
咨询类型：
     
*姓名：
*电话：
*单位：
Email：
*留言内容：
请详细说明您的需求。
*验证码：
 
AG 556
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
AG 556图片
CAS NO:133550-41-1
包装与价格：
包装价格(元)
10mg电议
50mg电议

产品介绍
AG 556 是一种高度选择性的 EGFR 抑制剂，还可以阻断 LPS 诱导的 TNF-α；生产。
Cas No.133550-41-1
别名(E)-Tyrphostin AG 556
化学名(E)-2-cyano-3-(3,4-dihydroxyphenyl)-N-(4-phenylbutyl)acrylamide
Canonical SMILESO=C(/C(C#N)=C/C(C=C1O)=CC=C1O)NCCCCC2=CC=CC=C2
分子式C20H20N2O3
分子量336.39
溶解度<10.09mg/ml in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

AG 556 is a selective inhibitor of EGFR with IC50 value of 1.1 μM.

The epidermal growth factor receptor (EGFR) is the cell-surface receptor for epidermal growth factor and plays an important role in tumor invasion and cancer cell proliferation.

AG 556 is a selective EGFR inhibitor. In HEK 293 cells expressing KIR2.3 or Kir2.1, AG556 (10 μM) reversibly reduced KIR2.3 or Kir2.1 currents. Also, AG556 inhibited tyrosine phosphorylation of KIR2.3 or Kir2.1 channels. EGF (100 ng/ml) increased KIR2.3 current, while this effect was inhibited by AG556 [1] [2]. AG556 arrested cells at G1/S phase by 85% and inhibited the activation of Cdk2 by phosphorylating tyrosine 15 on Cdk2 [3].

In a canine model infected with Escherichia coli 0111: B4, AG 556 increased survival times. AG 556 increased mean arterial pressure, oxygen delivery, cardiac output, alveolar-arterial oxygen gradient and left ventricular ejection fraction, which suggested that AG 556 increased survival. Also, AG 556 significantly reduced the levels of serum TNF, which suggested that AG 556 inhibited cell-signaling pathways and cytokine-induced multiorgan failure [4].

References:
[1].  Zhang DY, Zhang YH, Sun HY, et al. Epidermal growth factor receptor tyrosine kinase regulates the human inward rectifier potassium K(IR)2.3 channel, stably expressed in HEK 293 cells. Br J Pharmacol, 2011 Nov, 164(5): 1469-1478 [1].
[2].  Zhang DY, Wu W, Deng XL, et al. Genistein and tyrphostin AG556 inhibit inwardly-rectifying Kir2.1 channels expressed in HEK 293 cells via protein tyrosine kinase inhibition. Biochim Biophys Acta, 2011, 1808(8): 1993-1999.
[3].  Kleinberger-Doron N, Shelah N, Capone R, et al. Inhibition of Cdk2 activation by selected tyrphostins causes cell cycle arrest at late G1 and S phase. Exp Cell Res, 1998, 241(2): 340-351.
[4].  Sevransky JE, Shaked G, Novogrodsky A, et al. Tyrphostin AG 556 improves survival and reduces multiorgan failure in canine Escherichia coli peritonitis. J Clin Invest, 1997, 99(8): 1966-1973.