Apatinib (YN968D1) is a potent inhibitor of VEGFR2 (1 nM), RET (13 nM), VEGFR1 (70 nM), KIT (429 nM), CYP2C9 (440 nM), SRC (530 nM), PDGFRB (537 nM), PDGFRA (>1000 nM), CYP3A4 (1800 nM), EGFR (>10000 nM), HER2 (>10000 nM), FGFR1 (>10000 nM), HLM (480000 nM), RLM (950000 nM). Apatinib (YN968D1) exhibits the greatest inhibitory potency toward VEGFR2 (IC50 = 1 nM).