1. Protein Tyrosine Kinase/RTK
  2. VEGFR
    c-Kit
    PDGFR

Anlotinib (Synonyms: AL3818)

Cat. No.: HY-19716 Purity: 99.65%
Handling Instructions

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

For research use only. We do not sell to patients.

Anlotinib Chemical Structure

Anlotinib Chemical Structure

CAS No. : 1058156-90-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 242 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 220 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 380 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 1300 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 2100 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Anlotinib 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 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 (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. HEC1B cells have an IC50 value of 46 μM, and MFE296 cells are sensitive to Anlotinib, 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 (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, only 5 of the 11 mice are found to have residual tumor burden at the end of the treatment period. Treatment with Anlotinib decreases neoangiogenesis by 48.5% and cell proliferation by 27% when compare with the control group[2].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.4543 mL 12.2717 mL 24.5435 mL
5 mM 0.4909 mL 2.4543 mL 4.9087 mL
10 mM 0.2454 mL 1.2272 mL 2.4543 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[2]

AN3CA (1.2×104 cells/well), HEC1B (104 cells/well), MFE280 (104 cells/well), HEC1A (104 cells/well), KLE (1.2×104 cells/well), MFE296 (8×103 cells/well), and Ishikawa cells (6×103 cells/well) are seeded in 96-well plates and incubated for 24 hours at 37°C in 5% CO2. Cells are treated with Anlotinib (AL3818) (range of concentrations from 0 to 100 μM) for 72 hours. Following Anlotinib treatments, cell numbers are determined by sulforhodamine B (SRB) assay. Measurements are taken from 3 independent experiments conducted in triplicate[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Anlotinib (AL3818) is solubilized in dimethyl sulfoxide 1%.

Mice are randomly assigned into 4 experimental groups as follows: control (dimethyl sulfoxide 1%) (n=4), Anlotinib (AL3818) (5 mg/kg per day) (n=11). AL3818 is administered daily through oral gavage. Mice are monitored and weighted daily over the course of 29 days. Animals are killed on day 29, and tumors are collected and weighted. Tumors are measured using electronic calipers, and tumor volume is calculated according to the following formula:length×width×height)/2[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

407.44

Formula

C₂₃H₂₂FN₃O₃

CAS No.

1058156-90-3

SMILES

CC(N1)=CC2=C1C=CC(OC3=CC=NC4=CC(OCC5(N)CC5)=C(OC)C=C43)=C2F

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 44 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
Anlotinib
Cat. No.:
HY-19716
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