Altogether, it is for the first time we report that SP1049C therapy decreases the tumorigenicity and aggressiveness of cancer cells in vivo, suppresses the Wnt-β-catenin signaling activation and BCRP overexpression, differentially alters the DNA methylation profiles, as well as depletes the tumorigenic cell subpopulations in murine leukemia model. This evidence concerns the gene ABCG2 and cancer.