AIM: To investigate antitumor effect of allotri-tridecyl diethylamine (D-108) in vivo and in vitro. METHODS: The cytotoxic effects of D-108 on various tumor cell lines, human gingival fibroblast and marrow stromal cell cultured in vitro were determined with trypan blue dye exclusion test and MTT method. The acute toxicity of mice by administration of D-108 was evaluated by Bliss method. At a tolerable dose level, D-108 was administrated to treat transplanted solid tumor U14, and tumor weight inhibition was observed. Apoptosis morphological transformation of HL 60 cell induced by D-108 was detected by the Giemsa staining. RESULTS: The cytotoxic effects in vitro of D-108 on various tumor cell lines (IC_ 50 : 0.22 to 2.19 mg?L~ -1 ) were more powerful than both human gingival fibroblast and marrow stromal cell (IC_ 50 : 5.55 and 3.57 mg?L~ -1 ). LD_ 50 of D-108 was 36.49 mg?kg~ -1 (mice, i.g.). D-108 inhibited in vivo growth of implanted solid tumor U14 of mice effectually. The inhibition rate of tumor weight of D-108 (100 mg?kg~ -1 ?d~ -1 i.g.) was 45.27 %. HL 60 cell appearanced typical apoptosis morphological transformation induced by D-108. CONCLUSION: D-108 had obvious antitumor activity in vivo and in vitro and little toxicity. D-108 could induce the apoptosis of HL 60 cell.