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Combretastatin A-1

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Catalog No. T36848Cas No. 109971-63-3
Alias Combretastatin A1

Combretastatin A-1 is a potent microtubule inhibitor with anti-tumour and anti-vascular activity, acting through microtubule protein depolymerisation-mediated inactivation of AKT to inhibit the Wnt/β-catenin pathway, and can be used to study hepatocellular carcinoma.

Combretastatin A-1

Combretastatin A-1

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Purity: 97.49%
Catalog No. T36848Alias Combretastatin A1Cas No. 109971-63-3
Combretastatin A-1 is a potent microtubule inhibitor with anti-tumour and anti-vascular activity, acting through microtubule protein depolymerisation-mediated inactivation of AKT to inhibit the Wnt/β-catenin pathway, and can be used to study hepatocellular carcinoma.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$35-In Stock
1 mL x 10 mM (in DMSO)$895 days5 days
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:97.49%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Combretastatin A-1 is a potent microtubule inhibitor with anti-tumour and anti-vascular activity, acting through microtubule protein depolymerisation-mediated inactivation of AKT to inhibit the Wnt/β-catenin pathway, and can be used to study hepatocellular carcinoma.
Targets&IC50
BGC-823 cells:12.2 nM, MDA-MB-231 cells:17.6 nM, NCI-1975 cells:256.3 nM, LM-3:33.8 nM, A375 cells:61 nM, Hepa1-6:32.9 nM, HepG2 cells:9.2 nM, Huh7 cells:728.2 nM, MCF-7 cells:46.0 nM, SMMC-7721 cells:12.8 nM, Bel-7402 cells:38.4 nM, CT-26:1075 nM
In vitro
Combretastatin A-1 (CA1P) induces apoptosis of TAMs in vitro through the same mechanism observed in HepG2 cells, and it eliminates TAMs in the tumor microenvironment (TME) in vivo. Combretastatin A-1 (1-10 nM; 24 hours) induces AKT inactivation and removal of GSK-3β inhibition by microtubule depolymerization, leading to HepG2 cell apoptosis [2]. Combretastatin A-1 (1-50 nM; 6 hours) reduces the mitochondrial membrane potential (MMP) of HepG2 cells and induces the accumulation of ROS in a dose-dependent manner [3].
In vivo
In the HepG2 subcutaneous xenograft model, Combretastatin A-1 (1-4 mg/kg; i.v. every other day for 4 weeks) significantly reduces the tumor volume [3].
In the orthotopic hepatocellular carcinoma mouse model, Combretastatin A-1 (2 mg/kg; every other day for 21 days) demonstrates enhanced apoptosis [3].
SynonymsCombretastatin A1
Chemical Properties
Molecular Weight332.35
FormulaC18H20O6
Cas No.109971-63-3
SmilesCOc1ccc(\C=C/c2cc(OC)c(OC)c(OC)c2)c(O)c1O
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 80 mg/mL (240.71 mM), Sonication is recommended.
DMF: 5 mg/mL (15.04 mM), Sonication is recommended.
Ethanol: 3 mg/mL (9.03 mM), Sonication is recommended.
DMSO:PBS (pH 7.2) (1:1): 0.5 mg/mL (1.5 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (9.93 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
Ethanol/DMF/DMSO
1mg5mg10mg50mg
5 mM0.6018 mL3.0089 mL6.0178 mL30.0888 mL
DMF/DMSO
1mg5mg10mg50mg
10 mM0.3009 mL1.5044 mL3.0089 mL15.0444 mL
DMSO
1mg5mg10mg50mg
20 mM0.1504 mL0.7522 mL1.5044 mL7.5222 mL
50 mM0.0602 mL0.3009 mL0.6018 mL3.0089 mL
100 mM0.0301 mL0.1504 mL0.3009 mL1.5044 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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