ART838 is a dimeric pimeloyl urea compound notable for its potent anti-leukemic activity and favorable pharmacological properties. In vitro, ART-838 exhibits submicromolar inhibitory concentrations against all leukemia cell lines, demonstrating anti-leukemic efficacy 88 times greater than artemether. This compound remains in the body for extended periods and works synergistically with other anti-leukemic agents and novel kinase inhibitors to suppress leukemia cell growth. In immunodeficient NOD-SCID-IL2Rgnull (NSG) mice, ART-838 attains a plasma half-life longer than that of artemether, sustaining effective anti-leukemic concentrations for over 8 hours. Intermittent ART-838 treatment notably inhibited the growth of acute leukemia xenografts and primary grafts in NSG mice, surpassing the efficacy of artemether.