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Anti-ITGA2 (Vatelizumab)-SPDB-DM4 ADC (ADC-W-1455)

This ADC product is comprised of an anti-ITGA2 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
  • ITGA2
  • Alternative Names
  • ITGA2; integrin, alpha 2 (CD49B, alpha 2 subunit of VLA-2 receptor); CD49B; integrin alpha-2; CD49b; integrin alpha 2; collagen receptor; VLA-2 subunit alpha; platelet antigen Br; platelet glycoprotein Ia; platelet glycoprotein GPIa; CD49 antigen-like family member B; platelet membrane glycoprotein Ia; very late activation protein 2 receptor, alpha-2 subunit; BR; GPIa; VLA-2; VLAA2; BDPLT9;
  • Target Entrez Gene ID
  • 3673
  • Overview
  • This gene encodes the alpha subunit of a transmembrane receptor for collagens and related proteins. The encoded protein forms a heterodimer with a beta subunit and mediates the adhesion of platelets and other cell types to the extracellular matrix. Loss of the encoded protein is associated with bleeding disorder platelet-type 9. Antibodies against this protein are found in several immune disorders, including neonatal alloimmune thrombocytopenia. This gene is located adjacent to a related alpha subunit gene. Alternative splicing results in multiple transcript variants.

 ADC Antibody

  • Overview
  • Humanized Anti-ITGA2 IgG4-kappa antibody, Vatelizumab
  • Generic name
  • Vatelizumab

 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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