| 应用 |
A protein tyrosine kinase inhibitor with potent effects on TrkA |
| 产品介绍 |
AG879是酪氨酸激酶的抑制剂，能够抑制TrKA的磷酸化，但不能抑制TrKB 和TrKC，也是高选择性的ErbB2激酶抑制剂。 |
| 备注 |
Tyrphostin AG 879 potently inhibits HER2/ErbB2 with IC50 of 1 μM, 100- and 500-fold higher selective to ErbB2 than PDGFR and EGFR. |
| 生化机理 |
Tyrphostin AG 879 is a protein tyrosine kinase inhibitor with potent effects on TrkA. This product reportedly inhibits NGF-induced PLC-γ 1 phosphorylation and phosphatidylinositol-3 kinase activation. Has been shown in lab studies to disrupt Sertoli cell aggregation and stop androgen-induced cell proliferation. AG 879 also displays anti-cancer effects by inhibiting the expression of RAF-1 gene encoding MAP kinase activity necessary for human breast cancer cell proliferation. Shown to inhibit Neu (HER-2 or ERBB2) expression and reduced tumor sizes in mice leukemia cells. Tyrphostin AG 879 is an inhibitor of Flk-1. |
| 别名 |
AG 879；AG-879；AG879;AG 879；AG-879；AG879； α-Cyano-(3,5-di-t-butyl-4-hydroxy)thiocinnamide； (E)-3-[3,5-Bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-cyano-2-propenethioamide |
