Anti-ERBB2 (Trastuzumab)-AO-Mc-MMAE (Glyco MMAE) ADC (ADC-W-392)

This ADC product is comprised of an anti-ERBB2 monoclonal antibody conjugated via a AO-Mc linker to a MMAE (Glyco 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
  • ERBB2
  • Alternative Names
  • ERBB2; erb-b2 receptor tyrosine kinase 2; NEU; NGL; HER2; TKR1; CD340; HER-2; MLN 19; HER-2/neu; receptor tyrosine-protein kinase erbB-2; herstatin; p185erbB2; proto-oncogene Neu; c-erb B2/neu protein; proto-oncogene c-ErbB-2; metastatic lymph node gene 1
  • Target Entrez Gene ID
  • 2064
  • Overview
  • This gene encodes a member of the epidermal growth factor (EGF) receptor family of receptor tyrosine kinases. This protein has no ligand binding domain of its own and therefore cannot bind growth factors. However, it does bind tightly to other ligand-bound EGF receptor family members to form a heterodimer, stabilizing ligand binding and enhancing kinase-mediated activation of downstream signalling pathways, such as those involving mitogen-activated protein kinase and phosphatidylinositol-3 kinase. Allelic variations at amino acid positions 654 and 655 of isoform a (positions 624 and 625 of isoform b) have been reported, with the most common allele, Ile654/Ile655, shown here. Amplification and/or overexpression of this gene has been reported in numerous cancers, including breast and ovarian tumors. Alternative splicing results in several additional transcript variants, some encoding different isoforms and others that have not been fully characterized.

 ADC Antibody

  • Overview
  • Humanized Anti-ERBB2 Antibody, Trastuzumab
  • Generic name
  • Trastuzumab
  • Species Reactivity
  • Human

 ADC Linker

  • Name
  • AO-Mc
  • 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
  • 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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