MD-224

Description

MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 MDM2 degrader based on the proteolysistargeting chimera PROTAC concept. MD-224 consists of ligands for Cereblon and MDM2. MD-224 induces rapid degradation of MDM2 at concentrations 1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent. MD-224 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition CuAAc with molecules containing Azide groups.