Anti-PCSK9 (Evolocumab)-MC-Vc-PAB-DMEA-(PEG2)-duocarmycin SA ADC (ADC-W-2383)

This ADC product is comprised of an anti-PCSK9 monoclonal antibody conjugated via a MC-Vc-PAB-DMEA-(PEG2) linker to duocarmycin SA. The duocarmycin SA is targeted to certain cancers by immunerecognition and delivered into cancer cells via receptor mediated endocytosis. Within the cell, duocarmycin SA binds to DNA, causes DNA damage.

 ADC Target

  • Name
  • PCSK9
  • Alternative Names
  • PCSK9; proprotein convertase subtilisin/kexin type 9; HCHOLA3, hypercholesterolemia, autosomal dominant 3; FH3; NARC 1; NARC1; NARC-1; HCHOLA3;
  • Target Entrez Gene ID
  • 353175
  • Overview
  • This gene encodes a member of the subtilisin-like proprotein convertase family, which includes proteases that process protein and peptide precursors trafficking through regulated or constitutive branches of the secretory pathway. The encoded protein undergoes an autocatalytic processing event with its prosegment in the ER and is constitutively secreted as an inactive protease into the extracellular matrix and trans-Golgi network. It is expressed in liver, intestine and kidney tissues and escorts specific receptors for lysosomal degradation. It plays a role in cholesterol and fatty acid metabolism. Mutations in this gene have been associated with autosomal dominant familial hypercholesterolemia. Alternative splicing results in multiple transcript variants.

 ADC Antibody

  • Overview
  • Human Anti-PCSK9 IgG2-lambda antibody, Evolocumab
  • Generic name
  • Evolocumab
  • Host animal
  • Human

 ADC Linker

  • Name
  • MC-Vc-PAB-DMEA-(PEG2)
  • 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
  • duocarmycin SA
  • Description
  • Duocarmycins SA belong to the minor-groove-binding DNA-alkylating agents (DNA MGBA). The natural duocarmycins are isolated from the culture broth of Streptmyces sp and a series of derivatives has also been synthesized.

For Research Use Only. NOT FOR CLINICAL USE.


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