产品描述:
Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which selectively inhibit PTKs of key growth factors.{14963} AG-879 is a tyrphostin compound that inhibits nerve growth factor (NGF)-dependent TrkA tyrosine phosphorylation in PC-12 cells (IC50 = ~40 μM), HER2-ErbB2 kinase in several breast and ovarian cancer cell lines (IC50 = ~0.5 μM), and the VEGF receptor FLK1 (IC50 = ~1 μM).{15153} Additionally, AG-879 inhibits the activation of ETK with an IC50 value of ~5 nM, which blocks tyrosine phosphorylation of PAK1, suppressing Ras transformation of NIH 3T3 fibroblasts.{19455} AG-879 has also been shown to suppress IL-6-induced tyrosine phosphorylation of STAT3 (IC50 = 15 μM) in schwannoma cells.{19454}