Abstract: The purpose of this article is to study the preparation and biodistribution of 188Re-DTPA-DG in nude mice bearing MCF-7 mammary cancer cell. DTPA-deoxyglucose (DTPA-DG) was synthesized by conjugating D-glucosamine to diethylenetriaminepentaacetic acid (DTPA), then radiolabeled with 188Re. The biodistribution of 88Re-DTPA-DG in nude mice bearing MCF-7 mammary cancer cell was studied. The result showed that the radiolabeling yield of 188Re-DTPA-DG was 95.0%. The tumor-to-muscle ratio at 12h post intravenous injection was 12.76. 188Re-DTPA-DG showed excellent tumor targeting.