REVIEW Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM, >40-fold selective for VEGFR2 than c-Kit, PDGFR-alfa and FGFR-2, little activity to EGFR, HGFR and InsR. IC50 value: 0.9 nM. Target: VEGFR2 in vitro: Ki8751 potently and selectively inhibits VEGFR2 with IC50 of 0.9 nM. Ki8751 also inhibits PDGFR-alfa, c-Kit, and FGFR-2, with much higher IC50 values (40 nM-170 nM). Except for these several kinases, Ki8751 doesn''t disturb other kinases, including HGFR, EGFR, and InsulinR, even at 10 µM. In human umbilical vein endothelial cells (HUVECs), Ki8751 (1 nM-100 nM) effectively decreases VEGF-stimulated cell proliferation and vasculature permeability. In metastatic colorectal cancer (CRC) cells MIP, RKO, SW620, and SW480, but not in HCT116, Ki8751 (10 nM) increases cellular senescence. in vivo: In nude mice bearing human tumor xenografts of GL07, St-4, LC6, DLD-1, and A375 cells, Ki8751 (20 mg/kg) inhibits tumor growth. In nude rat xenograft models of LC-6 cells, Ki8751 (5 mg/kg) completely inhibits tumor growth without affecting body weight.
REFERENCES
[1]
Hasan MR, et al. Inhibition of VEGF induces cellular senescence in colorectal cancer cells. Int J Cancer, 2011, 129(9), 2115-2123.
[2]
Tamura D, et al. Bortezomib potentially inhibits cellular growth of vascular endothelial cells through suppression of G2/M transition. Cancer Sci, 2010, 101(6), 1403-1408.
[3]
'Kubo K, et al. Novel potent orally active selective VEGFR-2 tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of N-phenyl-N''-{4-(4-quinolyloxy)phenyl}ureas. J Med Chem, 2005, 48(5), 1359-1366.'
[4]
Kubo, Kazuo; Journal of Medicinal Chemistry 2005, V48(5), P1359-1366
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