| Bioactivity | APE1-IN-2 (compound AP1) is a Pt(IV) prodrug, 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]. |
| Invitro | APE1-IN-2 (compound AP1) can strongly inhibit the growth of malignant cells, including Cisplatin-resistant cancer cells, with up to 18.11 times inhibition compared with Cisplatin (HY-17394)[1].APE1-IN-2 (500 nM, 24 h) arrests the cell cycle in A549 and MCF7 cells[1].APE1-IN-2 (10 μM, 24 h) induces p53-dependent apoptosis in A549 cells[1].APE1-IN-2 (0-250 μM, 72 h) inhibits AP-cutting activity with an IC50 of 45.14 ± 17.37 μM[1].APE1-IN-2 can directly inhibit the AP endonuclease activity of APE1, leading to an interruption of miRNA processing and upregulation of the tumor suppressor PTEN[1]. Cell Proliferation Assay[1] Cell Line: |
| 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: |
| Name | APE1-IN-2 |
| Formula | C9H12Cl2N4O5Pt |
| Molar Mass | 522.21 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |