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APE1-IN-2

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Catalog No. T73299Cas No. 2923433-95-6

APE1-IN-2 (compound AP1), a Pt(IV) proagent, selectively targets the essential base excision repair protein apurinic/apyrimidinic endonuclease 1 (APE1). Exhibiting anticancer properties, APE1-IN-2 prompts the intracellular accumulation of platinum and initiates the activation of DNA damage response and apoptosis pathways [1].

APE1-IN-2

APE1-IN-2

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Catalog No. T73299Cas No. 2923433-95-6
APE1-IN-2 (compound AP1), a Pt(IV) proagent, selectively targets the essential base excision repair protein apurinic/apyrimidinic endonuclease 1 (APE1). Exhibiting anticancer properties, APE1-IN-2 prompts the intracellular accumulation of platinum and initiates the activation of DNA damage response and apoptosis pathways [1].
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
25 mg$1,5208-10 weeks8-10 weeks
50 mg$1,9808-10 weeks8-10 weeks
100 mg$2,5008-10 weeks8-10 weeks
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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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Product Introduction

Bioactivity
Description
APE1-IN-2 (compound AP1), a Pt(IV) proagent, selectively targets the essential base excision repair protein apurinic/apyrimidinic endonuclease 1 (APE1). Exhibiting anticancer properties, APE1-IN-2 prompts the intracellular accumulation of platinum and initiates the activation of DNA damage response and apoptosis pathways [1].
In vitro
APE1-IN-2 (compound AP1) robustly suppresses malignant cell proliferation, including Cisplatin-resistant strains, exhibiting up to 18.11-fold greater inhibition than Cisplatin [1]. At 500 nM for 24 hours, it halts cell cycle progression in A549 and MCF7 cells [1], while at 10 μM for 24 hours, it induces p53-dependent apoptosis in A549 cells [1]. Additionally, APE1-IN-2 dose-dependently inhibits AP-cleavage activity with an IC50 of 45.14 ± 17.37 μM over 72 hours [1]. It directly targets APE1 endonuclease activity, disrupting miRNA processing and enhancing PTEN, a tumor suppressor gene expression [1].
In vivo
APE1-IN-2 (compound AP1) (2 mg/kg, IP, administered once every three days for 15 days) exhibits antitumor activity in the A549 xenograft model [1].
Chemical Properties
Molecular Weight522.21
FormulaC9H12Cl2N4O5Pt
Cas No.2923433-95-6
SmilesO=[N+](C1=CC=CC2=C1NC(C(O[Pt]([NH3])(Cl)(O)(Cl)[NH3])=O)=C2)[O-]
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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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:
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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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