Anlotinib hydrochloride

Description: Anlotinib is an orally available inhibitor of multiple tyrosine kinases, including human VEGFR1, VEGFR2, VEGFR3, PDGFRbeta, and c-Kit with IC50 values of 26.9, 0.2, 0.7, 115, and 14.8 nM, respectively. It demonstrates selectivity for these targets over others like c-Met, c-Src, HER2, and EGFR, which have IC50 values of >2,000 nM. Additionally, anlotinib effectively inhibits FGFR1 with an IC50 of 11.7 nM. Its anti-tumor activity has been confirmed in various cancer cell lines, including colorectal, renal, lung, breast, leukemia, melanoma, and glioblastoma, with IC50s ranging from 3-12.5 µM. Anlotinib also inhibits VEGF-induced endothelial cell migration (IC50= 0.1 nM) and FBS-induced tube formation, contributing to its anti-angiogenic effects. In vivo, it showed a significant reduction in tumor volume and angiogenesis in a SW620 xenograft mouse model at a dose of 3 mg/kg per day, highlighting its potential for cancer therapy. Target: Others. Smiles: O(C=1C2=C(C=C(OCC3(N)CC3)C(OC)=C2)N=CC1)C=4C(F)=C5C(=CC4)NC(C)=C5.Cl