Anti-ITGAV (Abituzumab)-SMCC-DM1 ADC (ADC-W-2438)

This ADC product is comprised of an anti-ITGAV monoclonal antibody conjugated via a SMCC linker to DM1. The DM1 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
  • ITGAV
  • Alternative Names
  • ITGAV; integrin, alpha V; antigen identified by monoclonal L230 , integrin, alpha V (vitronectin receptor, alpha polypeptide, antigen CD51) , MSK8, vitronectin receptor , VNRA, VTNR; integrin alpha-V; CD51; integrin alphaVbeta3; vitronectin receptor subunit alpha; antigen identified by monoclonal L230; integrin, alpha V (vitronectin receptor, alpha polypeptide, antigen CD51); MSK8; VNRA; VTNR; DKFZp686A08142;
  • Target Entrez Gene ID
  • 3685
  • Overview
  • The product of this gene belongs to the integrin alpha chain family. Integrins are heterodimeric integral membrane proteins composed of an alpha subunit and a beta subunit that function in cell surface adhesion and signaling. The encoded preproprotein is proteolytically processed to generate light and heavy chains that comprise the alpha V subunit. This subunit associates with beta 1, beta 3, beta 5, beta 6 and beta 8 subunits. The heterodimer consisting of alpha V and beta 3 subunits is also known as the vitronectin receptor. This integrin may regulate angiogenesis and cancer progression. Alternative splicing results in multiple transcript variants. Note that the integrin alpha 5 and integrin alpha V subunits are encoded by distinct genes.

 ADC Antibody

  • Overview
  • Humanized Anti-ITGAV IgG2-kappa antibody, Abituzumab
  • Generic name
  • Abituzumab
  • Host animal
  • Mouse

 ADC Linker

  • Name
  • SMCC (N-succinimidyl 4-(Nmaleimidomethyl)cyclohexane-1-carboxylate)
  • 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
  • DM1 (N2'-Deacetyl-N2'-(3-mercapto-1-oxopropyl)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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