Anti-ERBB3 (Duligotuzumab)-MC-Vc-PAB-SN38 ADC (ADC-W-2370)

This ADC product is comprised of an anti-ERBB3 monoclonal antibody conjugated via a MC-Vc-PAB linker to SN38. The SN-38 is targeted to certain cancers by immunerecognition and delivered into cancer cells via receptor mediated endocytosis. Within the cell, SN-38 binds to DNA, causes DNA damage.

 ADC Target

  • Name
  • ERBB3
  • Alternative Names
  • ERBB3; v-erb-b2 erythroblastic leukemia viral oncogene homolog 3 (avian); LCCS2, lethal congenital contracture syndrome 2; receptor tyrosine-protein kinase erbB-3; HER3; proto-oncogene-like protein c-ErbB-3; tyrosine kinase-type cell surface receptor HER3; LCCS2; ErbB-3; c-erbB3; erbB3-S; MDA-BF-1; c-erbB-3; p180-ErbB3; p45-sErbB3; p85-sErbB3; MGC88033;
  • Target Entrez Gene ID
  • 2065
  • Overview
  • This gene encodes a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases. This membrane-bound protein has a neuregulin binding domain but not an active kinase domain. It therefore can bind this ligand but not convey the signal into the cell through protein phosphorylation. However, it does form heterodimers with other EGF receptor family members which do have kinase activity. Heterodimerization leads to the activation of pathways which lead to cell proliferation or differentiation. Amplification of this gene and/or overexpression of its protein have been reported in numerous cancers, including prostate, bladder, and breast tumors. Alternate transcriptional splice variants encoding different isoforms have been characterized. One isoform lacks the intermembrane region and is secreted outside the cell. This form acts to modulate the activity of the membrane-bound form. Additional splice variants have also been reported, but they have not been thoroughly characterized.

 ADC Antibody

  • Overview
  • Humanized Anti-ERBB3 IgG1-kappa antibody, Duligotuzumab
  • Generic name
  • Duligotuzumab

 ADC Linker

  • Name
  • MC-Vc-PAB (maleimidocaproyl-valine-citrulline-p-aminobenzoyloxycarbonyl)
  • Description
  • Peptide linkers, belonging to Enzymatically cleavable linkers, combine greater systemic stability with rapid enzymatic release of the drug in the target cell. The scission of peptidic bonds relies on lysosomal proteolytic enzymes, which have very low activities in blood due to endogenous inhibitors and the unfavorably high pH value of blood.

 ADC payload drug

  • Name
  • SN-38 (7-ethyl-10-hydroxycamptothecin)
  • Description
  • SN38 (7-ethyl-10-hydroxy camptothecin) is an active metabolite of the cancer prodrug, irinotecan, with the ability of inhibiting Topoisomerase I, which is belong to the camptothecin family. SN-38 is formed via hydrolysis of irinotecan by carboxylesterases and metabolized via glucuronidation by UGT1A1.

For Research Use Only. NOT FOR CLINICAL USE.


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