Anlotinib (hydrochloride)

An orally bioavailable tyrosine kinase inhibitor that inhibits human VEGFR1, VEGFR2, VEGFR3, PDGFRβ, and c-Kit (IC50s = 26.9, 0.2, 0.7, 115, and 14.8 nM, respectively); selective for these kinases over c-Met, c-Src, HER2, and EGFR (IC50s = >2,000 nM); inhibits FGFR1 (IC50 = 11.7 nM); inhibits the growth of SW620 and HT-29 colorectal, 786-O and Caki-1 renal, A549 and NCI-H526 lung, MDA-MB-231 breast, HMC-1 leukemia, A375 melanoma, and U-87MG glioblastoma cancer cells (IC50s = 3-12.5 µM); inhibits VEGF-induced migration (IC50 = 0.1 nM) and FBS-induced tube formation in HUVECs; inhibits VEGF-induced angiogenesis in a CAM assay at 1.5 nmol; decreases tumor volume by 83% and tumor angiogenesis by 91.2% in a SW620 xenograft mouse model at 3 mg/kg per day