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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $45 | - | In Stock |
| 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]. |
| Molecular Weight | 371.52 |
| Formula | C19H21N3OS2 |
| Cas No. | 524708-03-0 |
| Smiles | CC(C)N1CCc2c(C1)sc(NC(C)=O)c2-c1nc2ccccc2s1 |
| Storage | store 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
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