Bexobrutideg (NX-5948) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. Bexobrutideg mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. Bexobrutideg is efficacious in a mouse collageninduced arthritis (CIA) model. Bexobrutideg can cross the blood brain barrier (BBB). Bexobrutideg is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: BTK ligand ( HY-170324 ); Blue: CRBN ligand ( HY-171893 ); Black: linker). (Pink: Btk ligand ( HY-170324 ); Blue: Cereblon ligand ( HY-171893 ); Black: linker).
Products | Products > Disease Areas > Inflammation or Immune System Disease | Products > Signaling Pathways > PROTAC | Products > Signaling Pathways > Protein Tyrosine Kinase/RTK | Products > Research Areas > Inflammation/Immunology | Products > Signaling Pathways > PROTACs | Products > Signaling Pathways > Btk
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