Objective To investigate antitumor effect of biaminotetradecanoic acid(D|82) in vivo and in vitro. Methods The cytotoxic effects of D|82 on various tumor cell lines cultured in vitro were determined by trypan blue dye exclusion test, MTT method and growth curve method. At a tolerable dose level, D|82 was administrated to treat transplanted solid tumors S180 and U14, tumor weight inhibition was observed. Results D|82 induced significant growth arrested in various malignant tumor cell lines cultured in vitro. IC-{50}of these cells exposed to the drug for 48 hours ranged from 2 to 5 μg/mL. D|82 inhibited in vivo growth of mice implanted solid tumor S180 and U14 in a dose|dependent manner. {Conclusion} D|82 had obvious antitumor activity in vivo and in vitro. D|82 is very hopeful to be a new antitumor drug.