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Anti-ITGAV+ITGB3 (Etaracizumab)-SPDB-DM4 ADC (CAT#: ADC-W-2127)

This ADC product is comprised of an anti-ITGAV+ITGB3 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
  • ADC Antibody
  • ADC Linker
  • ADC payload drug
  • Name
  • ITGAV+ITGB3
  • Alternative Names
  • ITGAV+ITGB3
  • Overview
  • Integrins are integral cell-surface proteins composed of an alpha chain and a beta chain. They are known to participate in cell adhesion as well as cell-surface mediated signalling. Integrins are heterodimeric integral membrane proteins composed of an alpha chain and a beta chain. CD51 encodes integrin alpha chain V. The I-domain containing integrin alpha V undergoes post-translational cleavage to yield disulfide-linked heavy and light chains, that combine with multiple integrin beta chains to form different integrins. Alpha-V integrins have been implicated in many developmental processes and are therapeutic targets for inhibition of angiogenesis and osteoporosis.
  • Overview
  • Humanized Anti-ITGAV+ITGB3 IgG1 antibody, Etaracizumab
  • Generic name
  • Etaracizumab
  • Host animal
  • Mouse
  • 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.
  • 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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