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AG 825
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 825图片
CAS NO:149092-50-2
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议

产品介绍
AG 825 (Tyrphostin AG 825) 是一种选择性和 ATP 竞争性 ErbB2 抑制剂，可抑制酪氨酸磷酸化，IC5\u200b\u200b0 为 0.35 μM。
Cas No.149092-50-2
别名酪氨酸磷酸化抑制剂AG825,Tyrphostin AG-825
化学名(E)-3-(3-((benzo[d]thiazol-2-ylthio)methyl)-4-hydroxy-5-methoxyphenyl)-2-cyanoacrylamide
Canonical SMILESOC(C(CSC1=NC2=CC=CC=C2S1)=CC(/C=C(C#N)/C(N)=O)=C3)=C3OC
分子式C19H15N3O3S2
分子量397.47
溶解度DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO: PBS (pH 7.2)(1:3): 0.1 mg/ml,Ethanol: 0.2 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 825 is a selective inhibitor of ErbB2 with IC50 values of 0.15 and 19 μM for ErbB2 and ErbB1 respectively [1].

Receptor tyrosine-protein kinase erbB-2 is a member of the human epidermal growth factor receptor family and promotes cell proliferation.

AG 825 is a selective ErbB2 inhibitor. AG825 inhibited autophosphorylation of HER2, HER1-2 and HER1 with IC50 values of 0.15, 0.35 and 19 μM, respectively [1]. In non-small cell lung cancer (NSCLC) cell lines expressing high-p185neu, the HER-2/neu gene product, AG825 significantly increased the chemosensitivities. However, AG825 with high concentrations inhibited the drug-induced G2 arrest and the activation of phosphorylated p34cdc2 [2]. In androgen-independent prostate cancer (PCa) cell lines C4 and C4-2, AG825 was toxic in a dose- and time-dependent way and inhibited phosphoactivation of HER-2/neu and its down-regulation. Also, AG825 induced an imbalance between p38 mitogen-activated protein kinase activation and extracellular signal-regulated kinase 1/2, which then led to p38-dependent apoptosis [3].

References:
[1].  Osherov N, Gazit A, Gilon C, et al. Selective inhibition of the epidermal growth factor and HER2/neu receptors by tyrphostins. J Biol Chem, 1993, 268(15): 11134-11142.
[2].  Tsai CM, Levitzki A, Wu LH, et al. Enhancement of chemosensitivity by tyrphostin AG825 in high-p185(neu) expressing non-small cell lung cancer cells. Cancer Res, 1996, 56(5): 1068-1074.
[3].  Murillo H, Schmidt LJ, Tindall DJ. Tyrphostin AG825 triggers p38 mitogen-activated protein kinase-dependent apoptosis in androgen-independent prostate cancer cells C4 and C4-2. Cancer Res, 2001, 61(20): 7408-7412.