Anlotinib (hydrochloride)

Anlotinib is 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).¹ It is selective for these kinases over c-Met, c-Src, HER2, and EGFR (IC₅₀s = >2,000 nM). It also inhibits FGFR1 (IC₅₀ = 11.7 nM for the human receptor).² Anlotinib 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-87 MG glioblastoma cancer cells (IC₅₀s = 3-12.5 μM).¹ It inhibits VEGF-induced migration (IC₅₀ = 0.1 nM) and FBS-induced tube formation in human umbilical vein endothelial cells (HUVECs). Anlotinib (1.5 nmol) inhibits VEGF-induced angiogenesis in a chicken chorioallantoic membrane (CAM) assay.² It also decreases tumor volume by 83% and tumor angiogenesis by 91.2% in a SW620 xenograft mouse model when administered at a dose of 3 mg/kg per day.¹

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1. Xie, C., Wan, X., Quan, H., et al. Preclinical characterization of anlotinib, a highly potent and selective vascular endothelial growth factor receptor-2 inhibitor. Cancer Sci. 109(4), 1207-1219 (2018).

2. Lin, B., Song, X., Yang, D., et al. Anlotinib inhibits angiogenesis via suppressing the activation of VEGFR2, PDGFRβ and FGFR1. Gene 654, 77-86 (2018).