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, Böhmer A, et al. Selective platelet-derived growth factor receptor kinase blockers reverse sis-transformation. Cancer Research, 1994, 54(23): 6106-6114.
[2] Kovalenko M, Rönnstrand 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.