Description General description Similar to but more potent than AG 1295 (Cat. No. 658550). A cell-permeable, reversible, and ATP-competitive, inhibitor of PDGF receptor kinase and blocks signaling of human PDGF α-receptors (IC50 = 1.0 µM) and β-receptors (IC50 = 800 nM) as well as of the related stem cell factor receptor c-kit (80% inhibition at 5 µM). Affects neither the binding of PDGF-BB to the PDGF-β receptor nor the receptor dimerization. Has no effect on autophosphorylation of the vascular endothelial growth factor receptor KDR or on DNA synthesis induced by vascular endothelial growth factor in porcine aortic endothelial cells. Also reverses the transformed phenotype of sis-transfected NIH/3T3 cells but has no effect on src-transformed NIH 3T3 cells or on the activity of the kinase p60c-src (F257) immunoprecipitated from these cells. Potently inhibits autophosphorylation in Flt3/Tel-BaF3 and Flt3/Itd-BaF3 cells with an IC50 of 300 nM and ~1 µM, respectively. Packaging 5 mg in Plastic ampoule Biochem/physiol Actions Cell permeable: yes Primary Target PDGFR kinase Product competes with ATP. Reversible: yes Target IC50: 1.0 µM, 800 nM, against signaling of human PDGF α-receptors, human PDGF β-receptors, respectively Warning Toxicity: Standard Handling (A) Reconstitution Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C. Other Notes Tse, KF., et al. 2002. Leukemia16, 2027. Tse, KF., et al. 2001. Leukemia15, 1001. Strutz, F., et al. 2001. Kidney Int.59, 579. Kovalenko, M., et al. 1997. Biochemistry 36, 6260. Kovalenko, M., et al. 1994. Cancer Res. 54, 6106.