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Anlotinib Dihydrochloride

Cat. No. M7530
Anlotinib Dihydrochloride Structure
Synonym:

AL3818 Dihydrochloride

Size Price Availability Quantity
5mg USD 450 In stock
10mg USD 650 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Protocol
Cell Experiment
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
Animal Experiment
Animal models Mice
Formulation dimethyl sulfoxide 1%
Dosages 5 mg/kg
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 480.36
Formula C23H24Cl2FN3O3
CAS Number 1360460-82-7
Purity >98%
Solubility 10 mM in DMSO
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Anlotinib Dihydrochloride, AL3818 Dihydrochloride supplier, VEGFR/PDGFR, inhibitors

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