Cell lines

Swiss 3T3 cells, porcine aortic endothelial cells, sis-transformed cells

Preparation method

The solubility of this compound in DMSO is >6.7mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

6-8 h

Applications

AG1296 (0.1-5 μM) dose-dependently inhibited the activity of PDGF receptor kinase in Swiss 3T3 cell membranes. AG1296 inhibited PDGF receptor autophosphorylation with an IC50 of 0.3-0.5 μM. AG1296 was also highly inhibitory towards PDGF-induced mitogenesis. AG1296 inhibited the mitogenic effect of basic FGF on Swiss 3D cells, albeit with an IC50 of 12.3 ± 3.1 μM. AG1296 potently inhibited PDGF-induced cell growth (IC50: 3.2 μM). In porcine aortic endothelial cells, AG1296 inhibited autophosphorylation of both human PDGFα- and PDGFβ-receptor and inhibited equipotently PDGFα- and PDGFβ-receptor -dependent DNA synthesis in cells transfected with either receptor. AG1296 (5-50 μM) potently inhibited the growth of the sis-transformed NIH 3T3 cells.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

Tyrphostin AG 1296 is a selective inhibitor of platelet-derived growth factor receptor (PDGFR) with IC50 value of 0.3μM-0.5μM [1].

Tyrphostin AG 1296 is an ATP-competitive inhibitor of PDGFR. It binds to PDGFR, causing a conformational change at the ATP-binding site. In the in vitro assay, it potently inhibits the ligand-induced autophosphorylation of PDGF receptor in Swiss 3T3 cell membranes. Tyrphostin AG 1296 does not affect the EGF receptor when the concentration is up to 100μM. Tyrphostin AG 1296 also inhibits the mitogenesis induced by PDGF but not EGF or insulin. It reversibly inhibits PDGF-induced DNA synthesis with a mean IC50 value of 1.5μM. Besides that, tyrphostin AG 1296 inhibits PDGF-induced cell growth with IC50 value of 3.2μM in Swiss 3T3 cells [1, 2].

References:
[1] Kovalenko M, Gazit A, Bohmer A, et al. Selective platelet-derived growth factor receptor kinase blockers reverse sis-transformation. Cancer Research, 1994, 54(23): 6106-6114.
[2] Kovalenko M, Ronnstrand L, Heldin C H, et al. Phosphorylation site-specific inhibition of platelet-derived growth factor β-receptor autophosphorylation by the receptor blocking tyrphostin AG1296. Biochemistry, 1997, 36(21): 6260-6269.