MD-4251

MD-4251 is an orally active MDM2 PROTAC degrader. MD-4251 potently degrades MDM2 in RS4;11 cells (DC50: 0.2 nM) and actives p53. MD-4251 shows strong antiproliferative activity against acute leukemia cells (wild-type p53) with minimal efficacy in mutant type. MD-4251 induces complete tumor regression in RS4;11 xenograft mice model[1]. Pink: MDM2 ligand ; Blue: CRBN ligase ligand (HY-W883326) ; Black: linker

C47H53Cl2FN8O4

883.88

O=C1NC2=CC(Cl)=CC=C2[C@]13C4(CCCCC4)N[C@H]([C@@H]3C5=CC=CC(Cl)=C5F)C(N[C@@H]6CC[C@H](CC6)CN7CCN(CC7)C8=CC=C9C(N(N=C9C%10C(NC(CC%10)=O)=O)C)=C8)=O

Casein Kinase; IKZF Family; MDM-2/p53; PROTACs

CK1; IKZF1; MDM2

Room temperature