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AG-213
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-213图片
CAS NO:122520-86-9
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
inhibitor of epidermal growth factor (EGF) receptor kinase
Cas No.122520-86-9
别名酪氨酸磷酸化抑制剂,Tyrphostin AG-213,Tyrphostin 47
化学名2-cyano-3-(3,4-dihydroxyphenyl)-2E-propenethioamide
Canonical SMILESN#C/C(=C\c1ccc(O)c(O)c1)/C(=S)N
分子式C10H8N2O2S
分子量220.2
溶解度≤10mg/ml in ethanol;20mg/ml in DMSO;15mg/ml in dimethyl formamide
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-213 is an inhibitor of protein tyrosine kinases (PTKs) and epidermal growth factor (EGF) receptor kinase [1,2].

Protein tyrosine kinases (PTKs) have been involved in regulating cell proliferation, cell differentiation, and signaling processes in the immune system. Dysfunction of protein tyrosine kinases result in inflammatory responses and diseases including cancer, atherosclerosis, and psoriasis [3]. The epidermal growth factor receptor (EGFR) is a transmembrane glycoprotein. Activation of EGFR results in autophosphorylation of receptor tyrosine kinase and has been involved in regulating cellular proliferation, differentiation, and survival. Overexpression of EGFR has been identified in a variety of tumor cell lines and has been associated with poor prognosis and decreased survival [4].

Administration of AG 213(100 μM) interfered with HUVEC focal adhesion and stress fiber formation. Pretreatment of monolayers with AG 213 (25, 50, and 75 μM) produced partial and incremental inhibition of HUVEC migration. In HUVEC, treatment with tyrphostin AG 213 (25 and 50 μM) demonstrated partial inhibition of stress fiber assembly compared with cells treated with 100 μM AG 213 [1]. AG 213 inhibited adhesion-associated tyrosine phosphorylation of pp125FAK activity in HUVEC [1]. AG-213 inhibited the activity of epidermal growth factor (EGF) receptor kinase with an IC50 value of 2.4 μM in the human epidermoid carcinoma cell line A431 [2].

References:
[1] Romer L H, McLean N, Turner C E, et al.  Tyrosine kinase activity, cytoskeletal organization, and motility in human vascular endothelial cells[J]. Molecular Biology of the Cell, 1994, 5(3): 349-361.
[2] Gazit A, Yaish P, Gilon C, et al.  Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors[J]. Journal of medicinal chemistry, 1989, 32(10): 2344-2352.
[3] Levitzki A, Gazit A.  Tyrosine kinase inhibition: an approach to drug development[J]. Science, 1995, 267(5205): 1782.
[4] Herbst R S.  Review of epidermal growth factor receptor biology[J]. International Journal of Radiation Oncology Biology Physics, 2004, 59(2): S21-S26.