Fruquintinib

VEGFR抑制剂（VEGFR1、VEGFR-2和VEGFR-3的IC50分别为33、35和0.5nM）；抑制253种激酶中的RET、FGFR1和c-Kit（IC50分别为128、181和458nM）；抑制VEGF-A诱导的HUVEC增殖和VEGF-C诱导的HLEC增殖（IC50分别为1.7和4.2nM）；在30和300nM时分别使HUVEC的管形成减少74%和94%；以每天0.5-20mg/kg的剂量持续21天，降低BGC-823、HT-29、Caki-1和NCIH460小鼠异种移植模型中的肿瘤生长。A VEGFR inhibitor (IC50s = 33, 35, and 0.5 nM for VEGFR1, -2, and -3, respectively); inhibits RET, FGFR1, and c-Kit (IC50s = 128, 181, and 458 nM, respectively) in a panel of 253 kinases; inhibits VEGF-A- induced proliferation of HUVECs and VEGF-C-induced proliferation of HLECs (IC50s = 1.7 and 4.2 nM, respectively); decreases tube formation by HUVECs by 74 and 94% at 30 and 300 nM, respectively; reduces tumor growth in BGC-823, HT-29, Caki-1, and NCI H460 mouse xenograft models at 0.5-20 mg/kg per day for 21 days.