tcsc0040093 Anlotinib Dihydrochloride

Anlotinib Dihydrochloride is a novel multi-target tyrosine kinase inhibitor that is designed to primarily inhibit VEGFR2/3, FGFR1-4, PDGFRα/β, c-Kit, and Ret.

IC50 & Target: VEGFR2/3, FGFR1-4, PDGFRα/β, c-Kit, Ret^[1]

In Vitro: Anlotinib Dihydrochloride is a novel multi-target tyrosine kinase inhibitor that is designed to primarily inhibit VEGFR2/3, FGFR1-4, PDGFRα/β, c-Kit, and Ret^[1]. The EC cell lines show differential sensitivity to Anlotinib Dihydrochloride (AL3818); AN3CA cells appear the most sensitive with an IC₅₀ value of 84 nM. The other cell lines are approximately 28- to 550-fold less sensitive to Anlotinib Dihydrochloride. HEC1B cells have an IC₅₀ value of 46 μM, and MFE296 cells are sensitive to Anlotinib Dihydrochloride, with an IC₅₀ value of 2.9 μM compare with 3.2, 28.9, 29, and 40 μM for Ishikawa, MFE280, KLE, and HEC1A, respectively^[2].

In Vivo: Within the Anlotinib Dihydrochloride (AL3818)-treated (5 mg/kg) group (n=11), tumor size is found to be reduced 26-fold, with an average tumor volume of 164.8±70 mm³, when compare with the control group. Following treatment with Anlotinib Dihydrochloride, only 5 of the 11 mice are found to have residual tumor burden at the end of the treatment period. Treatment with Anlotinib Dihydrochloride decreases neoangiogenesis by 48.5% and cell proliferation by 27% when compare with the control group^[2].