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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $1,520 | 8-10 weeks | 8-10 weeks | |
| 50 mg | $1,980 | 8-10 weeks | 8-10 weeks | |
| 100 mg | $2,500 | 8-10 weeks | 8-10 weeks |
| 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]. |
| Molecular Weight | 522.21 |
| Formula | C9H12Cl2N4O5Pt |
| Cas No. | 2923433-95-6 |
| Smiles | O=[N+](C1=CC=CC2=C1NC(C(O[Pt]([NH3])(Cl)(O)(Cl)[NH3])=O)=C2)[O-] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
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 ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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