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AG-183
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-183图片
CAS NO:122520-90-5
规格:98%
分子量:268.2
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:122520-90-5
分子式:C13H8N4O3
分子量:268.2
纯度:98%
存储:Store at -20°C

Background:

AG-183, a member of tyrphostin, is an inhibitor of protein tyrosine kinase [1].


Protein tyrosine kinase is an enzyme that catalyzes the transfer of the γ phosphate of ATP to tyrosine residues on protein substrates. Phosphorylation of proteins by kinases is an important mechanism in signal transduction and regulating cellular activity, such as cell division. Tyrosine phosphorylation is a key covalent modification that occurs in multicellular organisms as a result of intercellular communication during embryogenesis and maintenance of adult tissues. Phosphorylation of tyrosine residues modulates enzymatic activity and creates binding sites for the recruitment of downstream signaling proteins [2].


PTK inhibitors could preferentially inhibit the epidermal growth factor (EGF) receptor kinase to block EGF-dependent cell proliferation [1]. In the human epidermoid carcinoma cell line, A431AG-183 inhibited the activity of epidermal growth factor (EGF) receptor kinase with an IC50 value of 800 nM [1].


参考文献:
[1] 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.
[2] Hubbard S R, Till J H.? Protein tyrosine kinase structure and function[J]. Annual review of biochemistry, 2000, 69(1): 373-398.