Description
A potent multi-RTKs inhibitor of members of VEGFR and PDGFR families with IC50 of 4/3/3/14/4/66/190/170nM for KDR/FLT1/CSF1R/KIT/FLT3/PDGFRbeta/FLT4/Tie2, respectively; much less active (IC50>10uM) against other nonrelated tyrosine kinases, such as steroid receptor coactivator and EGFR; inhibits RTK phosphorylation (IC50=2, 4, and 7nM for PDGFRbeta, KDR, and CSF-1R, respectively) and VEGF-stimulated proliferation (IC50=0.2nM for human endothelial cells); exhibits efficacy in human fibrosarcoma and breast, colon, and small cell lung carcinoma xenograft models (ED50=1.5-5mg/kg, twice daily). Colon Cancer Phase 2 Discontinued