Additional file 1.
GW2580 potently inhibits c-Fms kinase and does not cross-react with other imatinib-targeted kinases at clinically relevant concentrations. (a, b) Cell-free kinase activity assay with time-resolved fluorescent readout for determination of the IC50 of imatinib and GW2580 for the kinases (a) Abl and (b) c-Kit. (c) Cell-based assay for determination of the IC50 of imatinib and GW2580 for c-Fms. Human peripheral blood mononuclear cells were treated with M-CSF in the presence of 0-10 μM GW2580 or imatinib for 48 hours. Macrophages were counted and values expressed relative to M-CSF treatment alone. (d) Cell-based assay for determination of the IC50 of imatinib and GW2580 for PDGFR. Fibroblast-like synoviocytes from a human RA patient were incubated with PDGF-bb in the presence of 0-30 μM GW2580 or imatinib. After 48 hours, FLS cultures were pulsed with [3H] thymidine for 18 hours. Values are expressed relative to PDGF-bb treatment. Data shown in a-d are representative of at least 2 independent experiments.
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Paniagua et al. Arthritis Research & Therapy 2010 12:R32 doi:10.1186/ar2940