Tyrphostin AG1296

Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC₅₀ of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC₅₀ in the micromolar range^[1][2][3]. IC50 & Target: IC50: 0.8 μM (PDGFR)^[1] In Vitro: Tyrphostin AG1296 (0.625-20 μM; 72 h) suppresses viability of PLX4032-resistant melanoma cells^[4].
Tyrphostin AG1296 (2.5-20 μM; 48 h) induces apoptosis of A375R cells^[4].
Tyrphostin AG1296 (5 and 20 μM; 2 h) inhibits PDGFR phosphorylation in A375R cells^[4].
Tyrphostin AG1296 (0.0625-1 μM; 8 h) inhibits migration of A375R cells^[4]. In Vivo: Tyrphostin AG1296 (40 and 80 mg/kg; i.p. daily for two weeks) suppresses A375R tumor growth in vivo^[4].
Tyrphostin AG1296 (2 mg/kg; i.p. every other day for 3 weeks) inhibits the atherosclerotic plaque progression and enhances plaque stability by inhibiting inflammatory responses, reducing the expression of matrix metalloproteinases and promoting macrophages from proinflammatory phenotype to anti-inflammatory phenotype^[5].