Ambamustine, also known as PTT-119, is a novel tripeptide anticancer agent. PTT 119 was demonstrated to have antileukemic activity on murine and human cell lines. Most leukemic cell populations appeared to be responsive to the drug in a dose-related fashion. By cluster analysis, it was possible to discriminate subsets of samples according to PTT 119 sensitivity, and to investigate cross resistance with cytosine arabinoside and daunorubicin. PTT 119 may deserve applications in the treatment of acute nonlymphoblastic leukemia patients.