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Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,520 | Backorder | |
50 mg | $1,980 | Backorder | |
100 mg | $2,500 | Backorder |
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 that of Cisplatin-resistant strains, exhibiting up to 18.11-fold greater inhibition than Cisplatin [1]. The compound at 500 nM for 24 hours halts cell cycle progression in A549 and MCF7 cells [1], while at 10 μM for 24 hours, it triggers p53-dependent apoptosis in A549 cells [1]. Additionally, APE1-IN-2 dose-dependently inhibits AP-cleavage activity with a half-maximal inhibitory concentration (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, once every three days for 15 days) demonstrates antitumor efficacy in the A549 xenograft model [1]. |
Molecular Weight | 522.21 |
Formula | C9H12Cl2N4O5Pt |
Cas No. | 2923433-95-6 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
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