MS154 is a first-in-class E3 ligase cereblon-recruited EGFR degrader with K d values of 1.8 nM and 3.8 nM for EGFR WT and EGFR L858R mutant, respectively. MS154 potently induces degradation of mutant, but not wild-type, EGFR in cancer cell lines in an E3 ligase-dependent manner. MS154 exhibits anticancer effects against lung cancer (blue: E3 ligase ligand ( HY-103596 ); black: linker ( HY-W096167 ); pink: EGFR ligand ( HY-168305 )). (Pink: EGFR ligand ( HY-168305 ); Blue: Cereblon ligand ( HY-103596 ); Black: linker ( HY-W096167 )).
Products | Products > Disease Areas > Cancer | Products > Disease Areas > Lung Cancer | Products > Signaling Pathways > PROTAC | Products > Signaling Pathways > Protein Tyrosine Kinase/RTK | Products > Signaling Pathways > JAK/STAT Signaling | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Research Areas > Cancer | Products > Signaling Pathways > PROTACs | Products > Signaling Pathways > EGFR
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