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

Anlotinib Dihydrochloride (Synonyms: AL3818 Dihydrochloride)

目录号: HY-19716A 纯度: 99.70%
产品使用指南

Anlotinib Dihydrochloride 是一种新型多靶点酪氨酸激酶抑制剂,主要用于抑制 VEGFR2/3FGFR1-4PDGFRα/βc-KitRet

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Anlotinib Dihydrochloride Chemical Structure

Anlotinib Dihydrochloride Chemical Structure

CAS No. : 1360460-82-7

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Size Price Stock Quantity
10 mM * 1 mL in DMSO ¥3850 In-stock
5 mg ¥3500 In-stock
10 mg ¥5000 In-stock
50 mg ¥15000 In-stock
100 mg ¥21000 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

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].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.0818 mL 10.4089 mL 20.8177 mL
5 mM 0.4164 mL 2.0818 mL 4.1635 mL
10 mM 0.2082 mL 1.0409 mL 2.0818 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 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. 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 Dihydrochloride (AL3818) is solubilized in dimethyl sulfoxide 1%.

Mice are randomly assigned into 4 experimental groups as follows: control (dimethyl sulfoxide 1%) (n=4), Anlotinib Dihydrochloride (AL3818) (5 mg/kg per day) (n=11). Anlotinib Dihydrochloride 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

480.36

Formula

C₂₃H₂₄Cl₂FN₃O₃

CAS No.

1360460-82-7

SMILES

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

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: 60 mg/mL (Need ultrasonic and warming)

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

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产品名称:
Anlotinib Dihydrochloride
目录号:
HY-19716A
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