Anti-TNF (Nerelimomab)-SPDB-DM4 ADC (ADC-W-1857)

 ADC Target

  • Name
  • TNF
  • Alternative Names
  • TNF; tumor necrosis factor; TNFA, tumor necrosis factor (TNF superfamily, member 2); DIF; TNF superfamily; member 2; TNF alpha; TNFSF2; TNF-a; cachectin; APC1 protein; TNF, monocyte-derived; TNF, macrophage-derived; TNF superfamily, member 2; tumor necrosis factor alpha; tumor necrosis factor-alpha; tumor necrosis factor ligand superfamily member 2; TNFA; TNF-alpha;
  • Target Entrez Gene ID
  • 7124
  • Overview
  • This gene encodes a multifunctional proinflammatory cytokine that belongs to the tumor necrosis factor (TNF) superfamily. This cytokine is mainly secreted by macrophages. It can bind to, and thus functions through its receptors TNFRSF1A/TNFR1 and TNFRSF1B/TNFBR. This cytokine is involved in the regulation of a wide spectrum of biological processes including cell proliferation, differentiation, apoptosis, lipid metabolism, and coagulation. This cytokine has been implicated in a variety of diseases, including autoimmune diseases, insulin resistance, and cancer. Knockout studies in mice also suggested the neuroprotective function of this cytokine.

 ADC Antibody

  • Overview
  • Humanized Anti-TNF IgG1 antibody, Nerelimomab
  • Generic name
  • Nerelimomab
  • Host animal
  • Mouse

 ADC Linker

  • Name
  • SPDB (N-succinimidyl-4-(2-pyridyldithio)butyrate)
  • Description
  • Disulfide Linkers, are extensively exploited as a chemically labile linkage. Since the release of disulfide-linked drugs requires a cytoplasmic thiol cofactor, such as glutathione (GSH). Disulfides maintain stable at physiological pH and only when ADCs are internalized inside cells, the cytosol provides reducing environment including intracellular enzyme protein disulfide isomerase, or similar enzymes, drugs can be released.

 ADC payload drug

  • Name
  • DM4 (N2'-Deacetyl-N2'-(4-mercapto-4-methyl-1-oxopentyl)maytansine)
  • Description
  • Derived from Maytansinoid,a group of cytotoxins structurally similar to rifamycin, geldanamycin, and ansatrienin. The eponymous natural cytotoxic agent maytansine is a 19-member lactam (ansa macrolide) structure originally isolated from the Ethiopian shrub Maytenus 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 cells.

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