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.
Target-Kategorie:
IKZF|||MDM-2/p53|||PROTACs|||Casein Kinase
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