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Beschreibung

A cell-permeable tetraamine compound that is identified from a computer-aided molecular docking screening based on Fak Y397 interaction and is shown to inhibit FAK (Cat. No. 324876) autophosphorylation as well as its kinase activity toward paxillin phosphorylation both in cell-free kinase assays (IC50<1 µ,M) and in BT474 breast cancer cultures, while exhibiting little activity against Pyk2 (Cat. No. 662067) autophosphorylation or the kinase activity of c-Raf, c-Src, EGFR, VEGFR-3, IGF-1, Met, PDGFR-alpha, Pyk2, and PI 3-K (p110delta/p85alpha). Reported to inhibit BT474 proliferation both in cultures in vitro (IC50 ~10 µ,M) and in mice in vivo (~25% of no treatment controls on day 23, 30 mg/kg via 5 i.p/wk)., A cell-permeable tetraamine compound that is identified from a computer-aided molecular docking screening based on Fak Y397 interaction and is shown to inhibit FAK autophosphorylation as well as its kinase activity toward paxillin phosphorylation both in cell-free kinase assays (IC50<1 M) and in BT474 breast cancer cultures, while exhibiting little activity against Pyk2 autophosphorylation or the kinase activity of c-Raf, c-Src, EGFR, VEGFR-3, IGF-1, Met, PDGFR-alpha, Pyk2, and PI 3-K (p110delta/p85alpha). Reported to inhibit BT474 proliferation both in cultures in vitro (IC50 ~10 M) and in mice in vivo (~25% of no treatment controls on day 23, 30 mg/kg via 5 i.p/wk).