Molecular Formula | C16H14N2O2 |
Molar Mass | 266.29 |
Density | 1.192±0.06 g/cm3(Predicted) |
Boling Point | 420.2±40.0 °C(Predicted) |
Solubility | Soluble in DMSO. |
Appearance | White solid |
Color | Yellow |
pKa | 0.48±0.30(Predicted) |
Storage Condition | Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
Sensitive | Light Sensitive |
In vitro study | AG1296 acts on Swiss 3T3 cells and porcine aortic endothelial cells to selectively inhibit PDGF receptor kinase and PDGF-dependent DNA synthesis, with 50% inhibition concentrations below 5 and 1 μm, respectively. AG1296 acted on Swiss 3T3 cells and inhibited FGFR and c-Kit with IC50 of 12.3 μm and 1.8 μm, respectively. AG1296 acts on porcine aortic endothelial cells and effectively inhibits human PDGF-α and-β receptor signaling pathways, but has no effect on autophosphorylation of VEGFR KDR or VEGF-induced DNA synthesis. AG1296 treatment reversed the transformation phenotype of sis-transfected NIH 3T3 cells, but had no effect on src-transformed NIH 3T3 cells. AG1296 is a competitive inhibitor of ATP. AG1296 interferes with PDGF binding or PDGF receptor dimerization and abrogates PDGF receptor autophosphorylation. Thus, AG1296 is a pure inhibitor of the catalytic activity of receptor tyrosine kinases. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.755 ml | 18.777 ml | 37.553 ml |
5 mM | 0.751 ml | 3.755 ml | 7.511 ml |
10 mM | 0.376 ml | 1.878 ml | 3.755 ml |
5 mM | 0.075 ml | 0.376 ml | 0.751 ml |
biological activity | Tyrphostin AG 1296 is a PDGFR inhibitor with IC50 of 0.3-0.5 μm, there was no inhibitory activity against EGFR. Tyrphostin AG 1296 is a PDGFR inhibitor with an IC50 of 0.3-0.5 μm and no inhibitory activity against EGFR. Tyrphostin AG1296 inhibited FGFR and c-Kit in Swiss 3T3 cells with IC50 values of 12.3 μm and 1.8 μm. Tyrphostin AG1296 can induce severe apoptosis in A375R cells. |
characteristics | AG1296 acts on normal and sis-transformed mouse fibroblasts and porcine aortic endothelial cells expressing human PDGF receptors, more potent and more specific than previously reported Tyrphostin-type inhibitors. |
Target | Value |
PDGFR | 0.3 μM-0.5 μM |
c-Kit (Swiss 3T3) | 1.8 μM |
FGFR (Swiss 3T3) | 12.3 μM |