Anti-MUC1 (Nacolomab tafenatox)-MC-MMAF ADC (ADC-W-1630)

 ADC Target

  • Name
  • MUC1
  • Alternative Names
  • MUC1; mucin 1, cell surface associated; mucin 1, transmembrane , PUM; mucin-1; CD227; PEM; episialin; DF3 antigen; H23 antigen; krebs von den Lungen-6; mucin 1, transmembrane; tumor-associated mucin; carcinoma-associated mucin; polymorphic epithelial muciMaytenus ovatus. Maytansinoids can bind to tubulin at or near the vinblastine-binding site, which interfere the formation of microtubules and depolymerize already formed microtubules, inducing mitotic arrest in the intoxicated
  • Target Entrez Gene ID
  • 4582
  • Overview
  • This gene encodes a membrane-bound protein that is a member of the mucin family. Mucins are O-glycosylated proteins that play an essential role in forming protective mucous barriers on epithelial surfaces. These proteins also play a role in intracellular signaling. This protein is expressed on the apical surface of epithelial cells that line the mucosal surfaces of many different tissues including lung, breast stomach and pancreas. This protein is proteolytically cleaved into alpha and beta subunits that form a heterodimeric complex. The N-terminal alpha subunit functions in cell-adhesion and the C-terminal beta subunit is involved in cell signaling. Overexpression, aberrant intracellular localization, and changes in glycosylation of this protein have been associated with carcinomas. This gene is known to contain a highly polymorphic variable number tandem repeats (VNTR) domain. Alternate splicing results in multiple transcript variants.

 ADC Antibody

  • Overview
  • Humanized Anti-MUC1 IgG1-Fab’ fragment, Nacolomab tafenatox
  • Generic name
  • Nacolomab tafenatox
  • Host animal
  • Mouse

 ADC Linker

  • Name
  • MC (maleimidocaproyl)
  • 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
  • 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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