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AG 825 Sale

(Synonyms: 酪氨酸磷酸化抑制剂AG825,Tyrphostin AG-825) 目录号 : GC13168

An inhibitor of Her2/Neu tyrosine kinase activity

AG 825 Chemical Structure

Cas No.:149092-50-2

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1mg
¥238.00
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5mg
¥816.00
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10mg
¥1,428.00
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50mg
¥5,099.00
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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.

Chemical Properties

Cas No. 149092-50-2 SDF
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 SMILES OC(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°C
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1 mM 2.5159 mL 12.5796 mL 25.1591 mL
5 mM 0.5032 mL 2.5159 mL 5.0318 mL
10 mM 0.2516 mL 1.258 mL 2.5159 mL
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