您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > AG 99
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 99
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 99图片
CAS NO:122520-85-8
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
AG 99 ((E)-Tyrphostin 46) 是一种有效的 EGFR 抑制剂。
Cas No.122520-85-8
别名酪氨酸磷酸化抑制剂A46,(E)-Tyrphostin 46; (E)-Tyrphostin AG 99
化学名(Z)-2-cyano-3-(3,4-dihydroxyphenyl)acrylamide
Canonical SMILESOC1=CC(/C=C(C#N)\C(N)=O)=CC=C1O
分子式C10H8N2O3
分子量204.18
溶解度DMF: 20 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
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 99 is a potent inhibitor of EGF receptor tyrosine kinase with IC50 value of 10 μM [1].

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 99 is a potent and competitive EGFR tyrosine kinase inhibitor against both the substrate polyGAT and ATP [1]. In serum-starved human bladder carcinoma cell line 5637 cells, the 145-kDa protein, which was the β-subunit of c-Met/hepatocyte growth factor (HGF) receptor, was phosphorylated on 1003, 1234 and 1235 tyrosine residues. Also, tyrosine kinases EGFR and Src were activated. While, AG99 or inhibitors of Src (PP2, SU6656) significantly inhibited tyrosine phosphorylation of p145met and induced cell death through activation of caspase-like proteases. These results suggested that serum-independent growth of 5637 cells was involved by the tyrosine phosphorylation of p145met mediated by Src and EGFR [2].

References:
[1].  Gazit A, Osherov N, Gilon C, et al. Tyrphostins. 6. Dimeric benzylidenemalononitrile tyrophostins: potent inhibitors of EGF receptor tyrosine kinase in vitro. J Med Chem, 1996, 39(25): 4905-4911.
[2].  Yamamoto N, Mammadova G, Song RX, et al. Tyrosine phosphorylation of p145met mediated by EGFR and Src is required for serum-independent survival of human bladder carcinoma cells. J Cell Sci, 2006, 119(Pt 22): 4623-4633.