产品描述:
VTP-50469 is an inhibitor of the protein-protein interaction between menin and mixed lineage leukemia 1 (MLL1) fusion proteins (Ki = 0.104 nM).{68745} It selectively inhibits the growth of ten leukemia cell lines expressing MLL1 fusion proteins (IC50s = 13-37 nM) over HL-60 , K562, and Reh leukemia cells expressing wild-type MLL1 (IC50s = >1,000 nM).{68746} VTP-50469 reduces MLL-AF9-induced increases in the expression of MLL fusion protein target genes, including MEIS1, MEF2C, JMJD1C, and PBX3, in MOLM-13 acute myeloid leukemia (AML) cells. In vivo, VTP-50469 (120 mg/kg twice per day) dramatically increases the survival of mice in a patient-derived xenograft (PDX) mouse model of B cell acute lymphoblastic leukemia (B-ALL).