Fruquintinib (1194506-26-7) is a potent and highly selective inhibitor of VEGFR kinase (IC50’s: VEGFR1= 33 nM, VEGFR2 = 35 nM, VEGFR3 = 0.5 nM).1 It potently inhibited VEGF/VEGFR signaling and cell proliferation in HUVECs and HLECs and prevented angiogenesis in vitro. Fruquintinib is currently is several clinical trials against metastatic colorectal cancer2 and nonsquamous non-small-cell lung cancer3.
1) Sun et al. (2014) Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1,2,3 tyrosine kinases for cancer therapy; Cancer Biol. Ther. 15 1635
2) Li et al. (2018) Effect of Fruquintinib vs Placebo on Overall Survival in Patients With Previously Treated Metastatic Colorectal Cancer: The FRESCO Randomized Clinical Trial; JAMA 319 2486
3) Lu et al. (2018) Randomized, Double-Blind, Placebo-Controlled, Multicenter Phase II Study of Fruquintinib After Two Prior Chemotherapy Regimens in Chinese Patients With Advanced Nonsquamous Non-Small-cell Lung Cancer; J. Clin. Oncol. 36 1207