AGL 2043 is a cell-permeable, tricyclic quinoxaline compound that acts as a potent, selective, ATP-competitive, and reversible inhibitor of type III receptor tyrosine kinases PDGFR (IC50 = 800 nM in 3T3 cells; 90 nM against purified PDGFβ-receptor), Flt-3/Flk-2 (Flt3), and c-Kit (Kit) (IC50 ~1-3 μM).Weakly inhibits PKA, EGFR, IGF-1R, VEGFR, and Src kinases (IC50 > 30 μM). Potently inhibits smooth muscle cell proliferation and balloon-induced stenosis in porcine heart.
1. Gazit, A., et al. 2003. Bioorg. Med. Chem. 11: 2007-2018. PMID: 12670652
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