Anti-TNFRSF8 (Brentuximab-HC-K133)-DBCO-MMAF ADC (ADC-W-250)

This ADC product is comprised of an anti-TNFRSF8 monoclonal antibody (Brentuximab variant,HC-K133) conjugated via a DBCO linker to MMAF. The MMAF is targeted to certain cancers by immunerecognition and delivered into cancer cells via receptor mediated endocytosis. Within the cell, MMAF 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
  • Anti-TNFRSF8 antibody, Brentuximab variant, HC-K133
  • Generic name
  • Brentuximab variant, HC-K133
  • Species Reactivity
  • Human

 ADC Linker

  • Name
  • DBCO (Dibenzocyclooctyl)
  • Description
  • Noncleavable linkers, is considered noncleavable-meaning linker cleavage, and payload release does not depend on the differential properties between the plasma and some cytoplasmic compartments. Instead, the release of the cytotoxic drug is postulated to occur after internalization of the ADC via antigen-mediated endocytosis and delivery to lysosomal compartment, where the antibody is degraded to the level of amino acids through intracellular proteolytic degradation.

 ADC payload drug

  • Name
  • MMAF (Monomethyl auristatin F)
  • 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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