Anti-TNFRSF8 (Brentuximab)-VC-PABC-MMAE ADC (ADC-W-509)

This ADC product is comprised of an anti-TNFRSF8 monoclonal antibody conjugated via a VC-PABC linker to MMAE. The MMAE is targeted to certain cancers by immunerecognition and delivered into cancer cells via receptor mediated endocytosis. Within the cell, MMAE binds to tubulins, interrupts microtubule dynamics, and subsequently, induces cell death.

 ADC Target

  • Name
  • TNFRSF8
  • Alternative Names
  • TNFRSF8; tumor necrosis factor receptor superfamily, member 8; CD30; Ki-1; D1S166E; tumor necrosis factor receptor superfamily member 8; Ki-1 antigen; CD30L receptor; cytokine receptor CD30; lymphocyte activation antigen CD30;
  • Target Entrez Gene ID
  • 943
  • Overview
  • The protein encoded by this gene is a member of the TNF-receptor superfamily. This receptor is expressed by activated, but not by resting, T and B cells. TRAF2 and TRAF5 can interact with this receptor, and mediate the signal transduction that leads to the activation of NF-kappaB. This receptor is a positive regulator of apoptosis, and also has been shown to limit the proliferative potential of autoreactive CD8 effector T cells and protect the body against autoimmunity. Two alternatively spliced transcript variants of this gene encoding distinct isoforms have been reported.

 ADC Antibody

  • Overview
  • Chimeric Anti-TNFRSF8 Antibody, Brentuximab
  • Generic name
  • Brentuximab
  • Species Reactivity
  • Human

 ADC Linker

  • Name
  • VC-PABC(valine-citrulline-p-aminobenzylcarbamate)
  • Description
  • Peptide linkers, belonging to Enzymatically cleavable linkers, combine greater systemic stability with rapid enzymatic release of the drug in the target cell. The scission of peptidic bonds relies on lysosomal proteolytic enzymes, which have very low activities in blood due to endogenous inhibitors and the unfavorably high pH value of blood.

 ADC payload drug

  • Name
  • MMAE (Monomethyl auristatin E)
  • Description
  • Derived from Auristatin,are water-soluble dolastatin analogs of dolastatin 10. Dolastatin 10 belongs to dolastatin family and it can powerfully bind to tubulin, thus inhibiting polymerization mediated through the binding to the vinca alkaloid binding domain, and causes cell to accumulate in metaphase arrest.

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