tyrphostin-ag-1296

Description: Tyrphostin AG 1296 (AG-1296) is a novel, potent, selective and ATP-competitive inhibitor of PDGFR with potential antitumor activity. It inhibits PDGFR with IC50 of 0.3-0.5 uM, it has no activity against EGFR. Tyrphostin AG 1296 acts by binding to PDGFR, which causes a conformational change at the ATP-binding site. In an 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 100uM. 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 1.5uM.

References: Cancer Res. 1994 Dec 1; 54(23):6106-14; Biochemistry. 1997 May 27; 36(21):6260-9.