Anti-CCL2 (Carlumab)-SPDB-DM4 ADC (ADC-W-753)

This ADC product is comprised of an anti-CCL2 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

  • Name
  • CCL2
  • Alternative Names
  • CCL2; chemokine (C-C motif) ligand 2; SCYA2, small inducible cytokine A2 (monocyte chemotactic protein 1, homologous to mouse Sig je); C-C motif chemokine 2; GDCF 2; HC11; MCAF; MCP 1; MCP1; MGC9434; monocyte chemoattractant protein 1; monocyte chemotactic and activating factor; monocyte chemotactic protein 1; homologous to mouse Sig je; monocyte secretory protein JE; small inducible cytokine subfamily A (Cys Cys); member 2; SMC CF; small-inducible cytokine A2; monocyte chemoattractant protein-1; small inducible cytokine subfamily A (Cys-Cys), member 2; small inducible cytokine A2 (monocyte chemotactic protein 1, homologous to mouse Sig-je); MCP-1; SCYA2; GDCF-2; SMC-CF; HSMCR30;
  • Target Entrez Gene ID
  • 6347
  • Overview
  • This gene is one of several cytokine genes clustered on the q-arm of chromosome 17. Chemokines are a superfamily of secreted proteins involved in immunoregulatory and inflammatory processes. The superfamily is divided into four subfamilies based on the arrangement of N-terminal cysteine residues of the mature peptide. This chemokine is a member of the CC subfamily which is characterized by two adjacent cysteine residues. This cytokine displays chemotactic activity for monocytes and basophils but not for neutrophils or eosinophils. It has been implicated in the pathogenesis of diseases characterized by monocytic infiltrates, like psoriasis, rheumatoid arthritis and atherosclerosis. It binds to chemokine receptors CCR2 and CCR4.

 ADC Antibody

  • Overview
  • Human Anti-CCL2 IgG1-kappa antibody, Carlumab
  • Generic name
  • Carlumab
  • Host animal
  • Human
  • Species Reactivity
  • 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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