The aim of this study was to investigate the molecular mechanisms of apoptosis induced by {2-[(3-Carboxy-1-oxopropyl) amino]-2-deoxy-D-Glucose} (COPADG) in the esophageal cancer cell line Eca-109 and to establish a relationship between the rate of apoptosis and Fas and Bcl-2 protein expression. Eca-109 cells were cultured under standard condition. Cell growth was measured by MTT assay. Apoptosis and cell proliferation were determined by flow cytometry. Expressions of apoptosis-regulated genes Fas and Bcl-2 were detected by immunohistochemical methods and image analysis. COPADG dose- and time-dependently inhibited the growth of Eca-109 cells in vitro. Incubation of Eca-109 cells with 40 μmol/l of COPADG for 48 h induced significant apoptosis. After drug treatment, Fas protein expression was increased, while Bcl-2 protein expression was decreased. COPADG is able to induce apoptosis in the esophageal cancer cell line Eca-109. The mechanism of apoptosis in these cells may be related to up-regulation of Fas gene expression and the down-regulation of Bcl-2, which may serve as the experimental evidence for development of new drugs for the non-surgical management of human esophageal cancer.