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APE1-IN-2 (compound AP1) is a Pt(IV) proagent, targeting a critical BER protein, apurinic/apyrimidinic endonuclease 1 (APE1). APE1-IN-2 shows anticancer activity. APE1-IN-2 induces intracellular accumulation of platinum and activates DNA damage response and apoptosis signals[1]. | [in vivo]
APE1-IN-2 (compound AP1) (2 mg/kg, IP, once every 3 days for 15 days) exhibits an antitumor effect on the A549 xenograft model[1]. | Animal Model: | BALB/c nude mice (5 week-old, female, 16 ± 2 g of body weight bearing A549 xenograft tumors)[1] | | Dosage: | 2 mg/kg | | Administration: | IP, once every 3 days for 15 days | | Result: | Exhibited a 3.86-fold xenograft tumor inhibitory activity compared to Cisplatin. Did not significantly alter the body weight of mice, improving its sufficient safety. |
| [References]
[1] Yuan Y, et al. Pt(IV) Prodrug as a Potential Antitumor Agent with APE1 Inhibitory Activity. J Med Chem. 2022 Nov 24;65(22):15344-15357. DOI:10.1021/acs.jmedchem.2c01318 |
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