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Anti-FN1 (Radretumab)-SMCC-DM1 ADC (ADC-W-1154)

This ADC product is comprised of an anti-FN1 sdAb 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
  • FN1
  • Alternative Names
  • FN1; fibronectin 1; fibronectin; CIG; cold insoluble globulin; FINC; GFND2; LETS; migration stimulating factor; MSF; cold-insoluble globulin; migration-stimulating factor; FN; FNZ; ED-B; GFND; DKFZp686H0342; DKFZp686I1370; DKFZp686F10164; DKFZp686O13149;
  • Target Entrez Gene ID
  • 2335
  • Overview
  • This gene encodes fibronectin, a glycoprotein present in a soluble dimeric form in plasma, and in a dimeric or multimeric form at the cell surface and in extracellular matrix. The encoded preproprotein is proteolytically processed to generate the mature protein. Fibronectin is involved in cell adhesion and migration processes including embryogenesis, wound healing, blood coagulation, host defense, and metastasis. The gene has three regions subject to alternative splicing, with the potential to produce 20 different transcript variants, at least one of which encodes an isoform that undergoes proteolytic processing. The full-length nature of some variants has not been determined.

 ADC Antibody

  • Overview
  • Human Anti-FN1 sdAb, Radretumab
  • Generic name
  • Radretumab
  • Host animal
  • Human

 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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