Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors specific for platelet-derived growth factor (PDGF) receptor kinase could help in the treatment of atherosclerosis, restenosis, pulmonary fibrosis, and gliomas.1 AG-1296 is a potent and selective inhibitor of PDGF receptor kinase with an IC50 value of about 0.4 µM both in vitro and in cells (Swiss 3T3 cells).2 It inhibits ligand-stimulated DNA synthesis in platelet-derived growth factor receptor and stem cell factor/kit receptor transfected cells with an IC50 values of 1.5 and 1.8 µM, respectively. 2 Treatment of sis oncogene transfected NIH3T3 cells with AG-1296 reverses the transformed phenotype.2WARNING This product is not for human or veterinary use.
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