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Anti-CTLA4 (Ipilimumab)-SPDB-DM4 ADC (CAT#: ADC-W-999)

This ADC product is comprised of an anti-CTLA4 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
  • CTLA4
  • Alternative Names
  • CTLA4; cytotoxic T-lymphocyte-associated protein 4; celiac disease 3 , CELIAC3; cytotoxic T-lymphocyte protein 4; CD; CD28; CD152; GSE; ICOS; CD152 isoform; celiac disease 3; cytotoxic T-lymphocyte antigen 4; cytotoxic T-lymphocyte-associated antigen 4; cytotoxic T-lymphocyte-associated serine esterase-4; cytotoxic T lymphocyte associated antigen 4 short spliced form; ligand and transmembrane spliced cytotoxic T lymphocyte associated antigen 4; GRD4; CTLA-4; IDDM12; CELIAC3;
  • Target Entrez Gene ID
  • 1493
  • Overview
  • This gene is a member of the immunoglobulin superfamily and encodes a protein which transmits an inhibitory signal to T cells. The protein contains a V domain, a transmembrane domain, and a cytoplasmic tail. Alternate transcriptional splice variants, encoding different isoforms, have been characterized. The membrane-bound isoform functions as a homodimer interconnected by a disulfide bond, while the soluble isoform functions as a monomer. Mutations in this gene have been associated with insulin-dependent diabetes mellitus, Graves disease, Hashimoto thyroiditis, celiac disease, systemic lupus erythematosus, thyroid-associated orbitopathy, and other autoimmune diseases.
  • Overview
  • Human Anti-CTLA4 IgG1-kappa antibody, Ipilimumab
  • Generic name
  • Ipilimumab
  • Host animal
  • Human
  • Species Reactivity
  • Human
  • 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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