Anti-IGF1R (Robatumumab)-SPDB-DM4 ADC (ADC-W-1251)

 ADC Target

  • Name
  • IGF1R
  • Alternative Names
  • IGF1R; insulin-like growth factor 1 receptor; CD221; IGFIR; IGFR; JTK13; MGC18216; IGF-I receptor; soluble IGF1R variant 1; soluble IGF1R variant 2; insulin-like growth factor I receptor; MGC142170; MGC142172;
  • Target Entrez Gene ID
  • 3480
  • Overview
  • This receptor binds insulin-like growth factor with a high affinity. It has tyrosine kinase activity. The insulin-like growth factor I receptor plays a critical role in transformation events. Cleavage of the precursor generates alpha and beta subunits. It is highly overexpressed in most malignant tissues where it functions as an anti-apoptotic agent by enhancing cell survival. Alternatively spliced transcript variants encoding distinct isoforms have been found for this gene.

 ADC Antibody

  • Overview
  • Human Anti-IGF1R IgG1-kappa antibody, Robatumumab
  • Generic name
  • Robatumumab
  • 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.

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