JWJ-01-378

JWJ-01-378 is a selective TRK PROTAC degrader. JWJ-01-378 efficiently degrades WT TRK and TPM3-TRKA fusion proteins and inhibits downstream pERK signaling, while showing limited efficacy against TRK inhibitor resistant mutants and ALK fusions. JWJ-01-378 potently suppresses cancer cell proliferation[1].Pink: TRK ligand ; Blue: CRBN ligase ligand (HY-103596) ; Black: linker

C55H62F2N10O9

1045.14

O=C(NCCCCCCCCNC(CN1CCN(CC1)C2=CC(NC3CCOCC3)=C(C=C2)C(NC4=NNC5=C4C=C(C=C5)CC6=CC(F)=CC(F)=C6)=O)=O)COC7=C8C(N(C(C8=CC=C7)=O)C9CCC(NC9=O)=O)=O

ERK; PROTACs; Trk Receptor

Room temperature