Tyrphostin AG1296

146535-11-7

266.29

DMSO : 33.33 mg/mL (125.16 mM; Need ultrasonic); H2O : < 0.1 mg/mL (insoluble)

Apoptosis; Protein Tyrosine Kinase/RTK; Protein Tyrosine Kinase/RTK; Protein Tyrosine Kinase/RTK

Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 uM. Tyrphostin AG1296 inhibits signaling of human PDGF alpha- and beta-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.
IC50 & Target: IC50: 0.8 uM (PDGFR)
In Vitro: Tyrphostin AG1296 (0.625-20 uM; 72 h) suppresses viability of PLX4032-resistant melanoma cells.

Tyrphostin AG1296 (2.5-20 uM; 48 h) induces apoptosis of A375R cells.

Tyrphostin AG1296 (5 and 20 uM; 2 h) inhibits PDGFR phosphorylation in A375R cells.

Tyrphostin AG1296 (0.0625-1 uM; 8 h) inhibits migration of A375R cells.
In Vivo: Tyrphostin AG1296 (40 and 80 mg/kg; i.p. daily for two weeks) suppresses A375R tumor growth in vivo.

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.