F-14512 Hydrochloride is a highly potent and tumor-selective inhibitor of DNA topoisomerase II. F-14512 Hydrochloride enhances topoisomerase II inhibition through the high affinity of polyamines for DNA, enabling selective cellular uptake. It exhibits significant cytotoxicity against tumor cells with high PTS activity and induces DNA damage and apoptosis. F-14512 Hydrochloride has demonstrated potent antitumor activity in various tumor models, including MX-1 breast cancer, HL-60 leukemia, and A2780 ovarian cancer. F-14512 Hydrochloride can be used in cancer treatment research.

Method: F-14512 Hydrochloride (1, 10, 100 μM) was incubated with ³²P-labeled c-myc DNA fragments and Topo II for 5 minutes; bands were detected by denaturing polyacrylamide gel electrophoresis and autoradiography.
Results: Clear cleavage bands were observed at 10 μM F-14512 Hydrochloride; F-14512 Hydrochloride strongly inhibited topoisomerase II activity even at lower concentrations. [1]
Method: Kelly cells were pretreated with F-14512 Hydrochloride (1 μM) for 6 hours, then harvested. Following harvest, the cells were irradiated with ionizing radiation (0, 2, 4, 6 Gy), cultured for 8–10 days post-irradiation, and the survival fraction was determined by clonogenic assay.
Results: F-14512 Hydrochloride significantly enhanced radiation sensitivity in Kelly cells.[2]

Methods: To investigate the antitumor activity of F-14512 Hydrochloride, female nude mice were subcutaneously inoculated with MX-1 human breast cancer cells and administered F-14512 Hydrochloride (0.16, 0.32, 0.63, 1.25, 2.5 mg/kg) intraperitoneally once daily, 5 days a week for 2 consecutive weeks, with observation continuing until day 46.
Results: F-14512 Hydrochloride (1.25 mg/kg) effectively inhibited tumor growth. [1]
Methods: To investigate the antitumor activity of F-14512 Hydrochloride (in a neuroblastoma liver metastasis model), female BALB/c nude mice were selected. SH-SY5Y-Luc#7 human neuroblastoma cells were injected via the tail vein. Following successful implantation, F-14512 Hydrochloride (1.25 mg/kg per dose) was administered intravenously, three times weekly for 2 consecutive weeks, with observation continuing until day 38.
Results: F-14512 Hydrochloride significantly inhibited tumor growth, with a maximum inhibition of 91%, and no weight loss (>2.5%) was observed; it was well tolerated.[2]