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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

🥰Excellent
Purity: 98.50%
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.
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1 mg$62In Stock
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Purity:98.50%
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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 | Shipping with blue ice.
Solubility Information
DMSO: 10 mg/mL (26.92 mM), Sonication is recommended.
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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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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