Fruquintinib (HMPL-013) is a potent and highly selective small molecule inhibitor of VEGFR1/2/3 with IC50 of 33/3/5/0.5 nM, respectively.
Fruquintinib (HMPL-013) weakly inhibits RET, FGFR-1 and c-kit kinases.
Fruquintinib (HMPL-013) demonstrates potent inhibition on VEGF-A dependent KDR phosphorylation in HEK293-KDR cells and VEGF-A induced proliferation in primary HUVECs with IC50 of 0.6 nM and 1.7 nM, respectively.
Fruquintinib (HMPL-013) suppresses tumor growth inhibition in a panel of tumor xenograft and patient derive xenograft models in mouse.
Fruquintinib (HMPL-013) is orally active.
