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Characteristics
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ABT-869 is multi-targeted inhibitor of all members of the VEGF and PDGF receptor families (e.g., KDR, IC50 value of 4 nM), but has much less activity (IC50 values >1 μM) against unrelated receptor tyrosine kinases, soluble tyrosine kinases or serine/threonine kinases. The kinase inhibition profile of ABT-869 is evident in cellular assays of RTK phosphorylation (IC50 values of 2, 4 and 7 nM for PDGFRbeta, KDR and CSF-1R, respectively) and VEGF-stimulated proliferation (0.2 nM IC50 for human endothelial cells).
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