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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
😃Good
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 Size | Price | Availability | Quantity |
|---|---|---|---|
| 25 mg | $1,520 | 8-10 weeks | |
| 50 mg | $1,980 | 8-10 weeks | |
| 100 mg | $2,500 | 8-10 weeks |
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Product Introduction
Bioactivity
Chemical Properties
| 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 |
Storage & Solubility Information
| Storage | Shipping with blue ice. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
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