1,2-Dimethyl-6-(2-thienyl)-imidazolo[5,4-g]quinoxaline
Tyrphostin AGL 2043 Yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. 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 PDGFb-receptor), Flt3, and Kit (IC50 = 1-3 µM). A weak inhibitor of PKA, EGFR, IGF-1R, VEGFR, and Src kinases (IC50 > 30 µM). Shown to be non-toxic. Potently inhibits smooth muscle cell proliferation and balloon-induced stenosis in pig heart. Displays enhanced aqueous solubility compared with its parent compound AG 1295 (Cat. No. 658550). Purity: ≥95% by HPLC. CAS 22617-28-8. Ref.: Gazit, A., et al. 2003. Bioorg. Med. Chem. 11, 2007. |
