An orally bioavailable pyrrolopyrimidinylurea compound that simultaneously binds to both the adenine and the adjacent hydrophobic pocket of the inactive form of VEGFR2 with high-affinity (type-II inhibitor) and acts as a pseudo-irreversible inhibitor with prolonged action. Shown to potently inhibit the activities of VEGFR2, VEGFR1, Tie-2, PDGFRa, PDGFRb and c-kit (IC50=6.2, 15, 20, 35, 96 and 170nM, respectively) with moderate to excellent selectivity over B-raf and Aurora-A (IC50=0.9 and 1.05uM) and FGFR1, HER2, EGFR, IR, PKCth (>10uM) among 18-kinases. Arrests VEGF-induced HUVECs proliferation (IC50=4.4uM) and suppresses DU145 carcinoma growth in a xenograft nude mouse model (6mg/kg, b.i.d.).
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