Anti-PCSK9 (Bococizumab)-MC-Vc-PAB-MMAE ADC (ADC-W-2231)

This ADC product is comprised of an anti-PCSK9 monoclonal antibody conjugated via a MC-Vc linker to MMAE. The MMAE is targeted to certain cancers by immunerecognition and delivered into cancer cells via receptor mediated endocytosis. Within the cell, MMAE binds to tubulins, interrupts microtubule dynamics, and subsequently, induces cell death.

 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
  • 255738
  • 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
  • Humanized Anti-PCSK9 IgG2-kappa antibody, Bococizumab
  • Generic name
  • Bococizumab
  • Host animal
  • Mouse

 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
  • MMAE
  • Description
  • Derived from Auristatin,are water-soluble dolastatin analogs of dolastatin 10. Dolastatin 10 belongs to dolastatin family and it can powerfully bind to tubulin, thus inhibiting polymerization mediated through the binding to the vinca alkaloid binding domain, and causes cell to accumulate in metaphase arrest.

For Research Use Only. NOT FOR CLINICAL USE.


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