PROTAC RET Degrader 1 (Compound 20) is an orally active and blood-brain barrier-crossing RET PROTAC degrader with DC 50 values for RET (WT) , RET (G810S) , RET (G810C) , and RET (G810R) of 1.7, 3, 12, and 21 nM, respectively. PROTAC RET Degrader 1 exhibits potent anti-proliferative activity in cancer cell lines carrying oncogenic RET fusions (such as KIF5B-RET, CCDC6-RET) or mutations (such as RET (C634W)). PROTAC RET Degrader 1 shows significant anti-tumor activity in human tumor xenograft (PDX) mouse models. PROTAC RET Degrader 1 can be used for the study of RET-positive cancers Pink: RET ligand ( HY-179308 ); Blue: CRBN ligand ( HY-179307 ); Black: Linker). (Pink: RET ligand ( HY-179308 ); Blue: Cereblon ligand ( HY-179307 ); Black: linker).
Products | Products > Disease Areas > Cancer | Products > Signaling Pathways > PROTAC | Products > Signaling Pathways > Protein Tyrosine Kinase/RTK | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Signaling Pathways > PROTACs | Products > Signaling Pathways > RET
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