Sunitinib is a potent inhibitor of CSF-1 receptor kinase in an enzyme assay, with an ICof 7 nM, and inhibits receptor phosphorylation in a cellular assay with an ICof 61 nM. Sunitinib inhibits SCF-induced phosphotyrosine levels on KIT (IC= 1 - 10 nM) and reduced SCF-stimulated ERK1/2 phosphorylation with an ICvalue consistent with that for inhibition of KIT phosphotyrosine levels. Sunitinib also inhibited SCF-stimulated proliferation in NCI-H526 cells (IC= 2 nM).
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