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. 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.
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.
|Cell lines||AN3CA, HEC1B, MFE280, HEC1A, KLE, MFE296 and Ishikawa cells|
|Preparation method||Cells are treated with Anlotinib Dihydrochloride (AL3818) (range of concentrations from 0 to 100 μM) for 72 hours. Following Anlotinib Dihydrochloride treatments, cell numbers are determined by sulforhodamine B (SRB) assay.|
|Concentrations||0 to 100 μM|
|Incubation time||72 hours|
|Formulation||dimethyl sulfoxide 1%|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
Anlotinib inhibits angiogenesis via suppressing the activation of VEGFR2, PDGFRβ and FGFR1.
Lin B, et al. Gene. 2018 May 15;654:77-86. PMID: 29454091.
Preclinical characterization of anlotinib, a highly potent and selective vascular endothelial growth factor receptor-2 inhibitor.
Xie C, et al. Cancer Sci. 2018 Apr;109(4):1207-1219. PMID: 29446853.
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