MD-4251

MD-4251 is an orally active MDM2 PROTAC degrader. It potently degrades MDM2 in RS4;11 cells (DC50: 0.2 nM) and activates p53. MD-4251 exhibits strong antiproliferative activity against acute leukemia cells with wild-type p53, but shows limited efficacy in mutant cells. In RS4;11 xenograft mouse models, MD-4251 induces complete tumor regression.