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O6-Benzylguanine

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Catalog No. T7539Cas No. 19916-73-5

O6-Benzylguanine is a guanine analog with antineoplastic activity,and is a potent O6-alkylguanine DNA alkyltransferase (AGT) inactivator.

O6-Benzylguanine

O6-Benzylguanine

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Purity: 98.90%
Catalog No. T7539Cas No. 19916-73-5
O6-Benzylguanine is a guanine analog with antineoplastic activity,and is a potent O6-alkylguanine DNA alkyltransferase (AGT) inactivator.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
25 mg$42In StockIn Stock
50 mg$62In StockIn Stock
100 mg$97In StockIn Stock
500 mg$233-In Stock
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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:98.90%
Appearance:Solid
Color:White
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Product Introduction

O6-Benzylguanine AI Summary
O6-Benzylguanine exhibits significant inhibitory activity against O6-alkylguanine-DNA alkyltransferase (AGT), also known as O6-methylguanine-DNA methyltransferase (MGMT), demonstrating potential as a therapeutic agent in cancer treatment, particularly breast cancer and colorectal carcinoma. In various cell lines, the compound shows effective inhibition with low IC50 and ED50 values, such as an ED50 of 0.2 µM and 0.05 µM in HT-29 cell-free extracts and HT-29 cells respectively. In MCF-7 breast cancer cells, it removes O6-methylguanine from DNA most effectively at 0.1 µM. Additionally, O6-Benzylguanine enhances the cytotoxicity of ACNU towards HeLa S3 cells with notable dose-modifying effects. Despite reduced effectiveness against certain AGT mutants, it maintains significant inactivation capacity in the presence of DNA. Beyond AGT inhibition, O6-Benzylguanine also displays bioactivity against the SARS-CoV-2 virus, inhibiting virus-induced cytotoxicity in VERO-6 cells, and it demonstrates weak myeloperoxidase inhibition while affecting multiple signaling and enzymatic pathways. Its inhibitory effects extend to aldehyde oxidase-mediated drug metabolism and myeloperoxidase activity, indicating broader pharmacological potential..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
O6-Benzylguanine is a guanine analog with antineoplastic activity,and is a potent O6-alkylguanine DNA alkyltransferase (AGT) inactivator.
Chemical Properties
Molecular Weight241.25
FormulaC12H11N5O
Cas No.19916-73-5
SmilesO(CC1=CC=CC=C1)C2=C3C(=NC(N)=N2)N=CN3
Relative Density.1.48 g/cm3 (Predicted)
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 60 mg/mL (248.7 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (8.29 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
DMSO
1mg5mg10mg50mg
1 mM4.1451 mL20.7254 mL41.4508 mL207.2539 mL
5 mM0.8290 mL4.1451 mL8.2902 mL41.4508 mL
10 mM0.4145 mL2.0725 mL4.1451 mL20.7254 mL
20 mM0.2073 mL1.0363 mL2.0725 mL10.3627 mL
50 mM0.0829 mL0.4145 mL0.8290 mL4.1451 mL
100 mM0.0415 mL0.2073 mL0.4145 mL2.0725 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:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

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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