STF-118804 reduces the viability of B-ALL cell lines containing MLL chromosomal translations, with IC50 values in the low nanomolar range. In addition, leukemic samples from five pediatric ALL patients are also sensitive to STF-118804 in the low nanomolar range. STF-118804 induces leukemia MV411 cell apoptosis without antecedent cell cycle arrest.
In vivo
STF-118804 (25 mg/kg twice daily, s.c.) improves survival in an orthotopic xenotransplant model of high-risk acute lymphoblastic leukemia, and effectively depletes leukemia-initiating cells.