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Aim: 3-bromopyruvate (3-BrPA) has antineoplastic activity on malignant cells.In this study, we investigated the toxicity of 3-BrPA on two breast cancer cell lines.Methods: The intracellular ATP level was measured by the ATP Assay Kit.Cell viability was measured using MTT assay.Cell death was assessed by flow cytometry with propidium iodide (PI) staining or PI/Annexin V staining.The ultrastructural details of two breast cancer cells treated with vehicle DMSO, 3-BrPA, or 3-BrPA plus caspase inhibitor (z-VAD-fmk) were analyzed by electron microscopy(EM).