Background: Pithecellobium dulce (Roxb.), an evergreen medium-sized, spiny tree which have vast nutritional values and widely used in ayurvedic medicines and home remedies. The plant has also been a rich source of biologically active compounds. The present study was designed to isolate pure compound and to know the efficacy as antioxidant as well as its anti-tumor activity on Ehrlich ascites carcinoma cell (EAC). Methods: The isolation of the compound was carried out by column chromatography and structure was revealed by 1H-NMR and 13C NMR. The antioxidant activity was investigated by the scavenging of 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radicals as well as the inhibition of oxidative damage of pUC19 plasmid DNA, hemolysis and lipid peroxidation induced by 2, 2’-azobis (2-amidinopropane) dihydrochloride (AAPH) in human erythrocytes. In vivo anti-tumor activity of the compound was also evaluated by determining the viable tumor cell count, hematological profiles of experimental mice along with observing morphological changes of EAC cells by fluorescence microscope. Results: The isolated compound showed strong antioxidant activity in DPPH radical scavenging with IC50 of 14.6μg/ml. It also effectively inhibited AAPH induced oxidation in DNA and human erythrocyte model and lipid per oxidation. In anti-tumor assay, 70.89±6.62% growth of inhibition of EAC was observed as compare to the control mice (p<0.05) at a dose 50mg/kg body weight. Conclusion: The compound may have a great importance as a therapeutic agent in preventing oxidative damage of biomolecules and therapeutic use in chemotherapy.