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APE1-IN-1

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Catalog No. T61487Cas No. 524708-03-0

APE1-IN-1 is a potent inhibitor of purine/pyrimidine endonuclease 1 (APE1) that crosses the blood-brain barrier, exhibits potential antitumor activity, and enhances the cytotoxicity of the alkylating agent [methyl methanesulfonate] on cancer cells.

APE1-IN-1

APE1-IN-1

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Purity: 98.5%
Catalog No. T61487Cas No. 524708-03-0
APE1-IN-1 is a potent inhibitor of purine/pyrimidine endonuclease 1 (APE1) that crosses the blood-brain barrier, exhibits potential antitumor activity, and enhances the cytotoxicity of the alkylating agent [methyl methanesulfonate] on cancer cells.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$32-In Stock
1 mL x 10 mM (in DMSO)$297-10 days7-10 days
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
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Batch Information

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Purity:98.5%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
APE1-IN-1 is a potent inhibitor of purine/pyrimidine endonuclease 1 (APE1) that crosses the blood-brain barrier, exhibits potential antitumor activity, and enhances the cytotoxicity of the alkylating agent [methyl methanesulfonate] on cancer cells.
Targets&IC50
qHTS assay:2 μM, Radiotracer incision assay:12 μM
In vitro
In the qHTS assay, APE1-IN-1 (compound 3) displays an IC50 of 2 μM, while in a radiotracer incision assay (RIA), it exhibits an IC50 of 12 μM[1].
In a dose-dependent manner, APE1-IN-1 (at concentrations of 0, 1, 3, 10, 30, or 100 μM for 15 minutes) inhibits AP site incision in HeLa whole cell extracts[1].
Furthermore, APE1-IN-1 (at concentrations ranging from 5 to 30 μM for 24 hours) demonstrates cytotoxic activity against HeLa cells and enhances the activity of methyl methansulfonate and Temozolomide[1].
In vivo
Administered at a single dosage of 30 mpk via intraperitoneal injection, APE1-IN-1 demonstrates favorable pharmacokinetic properties[1].
Chemical Properties
Molecular Weight371.52
FormulaC19H21N3OS2
Cas No.524708-03-0
SmilesCC(C)N1CCc2c(C1)sc(NC(C)=O)c2-c1nc2ccccc2s1
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: 10 mg/mL (26.92 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.69 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 mM2.6916 mL13.4582 mL26.9165 mL134.5823 mL
5 mM0.5383 mL2.6916 mL5.3833 mL26.9165 mL
10 mM0.2692 mL1.3458 mL2.6916 mL13.4582 mL
20 mM0.1346 mL0.6729 mL1.3458 mL6.7291 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

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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

Keywords

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