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Anti-TNFRSF9 (Urelumab)-SPDB-DM4 ADC (ADC-W-1893)

This ADC product is comprised of an anti-TNFRSF9 monoclonal antibody conjugated via a SPDB linker to DM4. The DM4 is targeted to certain cancers by immunerecognition and delivered into cancer cells via receptor mediated endocytosis. Within the cell, DM1 binds to tubulins, interrupts microtubule dynamics, and subsequently, induces cell death.

 ADC Target

  • Name
  • TNFRSF9
  • Alternative Names
  • TNFRSF9; tumor necrosis factor receptor superfamily, member 9; ILA; tumor necrosis factor receptor superfamily member 9; 4 1BB; CD137; CD137 antigen; T cell antigen ILA; T-cell antigen ILA; 4-1BB ligand receptor; homolog of mouse 4-1BB; receptor protein 4-1BB; T-cell antigen 4-1BB homolog; induced by lymphocyte activation (ILA); interleukin-activated receptor, homolog of mouse Ly63; 4-1BB; CDw137; MGC2172; FLJ43501;
  • Target Entrez Gene ID
  • 3604
  • Overview
  • The protein encoded by this gene is a member of the TNF-receptor superfamily. This receptor contributes to the clonal expansion, survival, and development of T cells. It can also induce proliferation in peripheral monocytes, enhance T cell apoptosis induced by TCR/CD3 triggered activation, and regulate CD28 co-stimulation to promote Th1 cell responses. The expression of this receptor is induced by lymphocyte activation. TRAF adaptor proteins have been shown to bind to this receptor and transduce the signals leading to activation of NF-kappaB.

 ADC Antibody

  • Overview
  • Human Anti-TNFRSF9 IgG4-kappa antibody, Urelumab
  • Generic name
  • Urelumab
  • Host animal
  • Human

 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.

For Research Use Only. NOT FOR CLINICAL USE.

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