Tyrphostin AG 1295 (CAS 71897-07-9)

Tyrphostin AG 1295 is a selective inhibitor of protein tyrosine kinases (PTKs). As a class of antiproliferative compounds it has demonstrated potent inhibitory effects in various cellular processes. In particular, Tyrphostin AG 1295 targeting PDGF (platelet-derived growth factor receptor)- receptor PTK, holds a great promise in the treatment of various diseases, including atherosclerosis, restenosis, pulmonary fibrosis, and gliomas. Additionally, AG1295, being a specific inhibitor of the PDGF receptor, exerts a significant inhibitory impact on the activation, migration, and proliferation of smooth muscle cells (SMCs) in vitro and autophosphorylation of PDGF receptor (R), specifically suppressing the enhancement caused by PDGF-BB without affecting the FGF-2 effect. AG-1295, a quinoxaline-type tyrphostin, exhibits potent and selective inhibition of PDGF receptor kinase both in vitro and in Swiss 3T3 cells (with IC50 values ranging from 0.3-1 µM). It effectively inhibits PDGF-stimulated DNA synthesis without affecting the activity of the EGF receptor. Notably, when delivered via biodegradable nanoparticles, It effectively attenuates PDGF-dependent DNA synthesis and inhibits neointimal formation after balloon injury in porcine femoral arteries. These compelling findings highlight the potential applicability of this novel therapeutic approach, warranting further investigations to evaluate its efficacy in interventional settings.