The CP-868,596 is a potent, oral, selective inhibitor of PDGFR-beta tyrosine kinase, with an IC 50 of 0.4 ng/ml while PDGFR-beta is commonly overexpressed in the stroma and pericytes of several solid organ tumour types. CP-868,596 is greater than 100-fold more selective for PDGFR than for other kinases, such as c-KIT, VEGFR-2, TIE-2, FGFR-2, EGFR, erbB2, and Src.
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