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Anti-TFPI (Concizumab)-MC-Vc-PAB-SN38 ADC (ADC-W-1794)

This ADC product is comprised of an anti-TFPI 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
  • TFPI
  • Alternative Names
  • TFPI; tissue factor pathway inhibitor (lipoprotein-associated coagulation inhibitor); LACI; tissue factor pathway inhibitor; EPI; extrinsic pathway inhibitor; TFI; TFPI1; anti-convertin;
  • Target Entrez Gene ID
  • 7035
  • Overview
  • This gene encodes a Kunitz-type serine protease inhibitor that regulates the tissue factor (TF)-dependent pathway of blood coagulation. The coagulation process initiates with the formation of a factor VIIa-TF complex, which proteolytically activates additional proteases (factors IX and X) and ultimately leads to the formation of a fibrin clot. The product of this gene inhibits the activated factor X and VIIa-TF proteases in an autoregulatory loop. Inhibition of the encoded protein restores hemostasis in animal models of hemophilia. This gene encodes multiple protein isoforms that differ in their inhibitory activity, specificity and cellular localization.

 ADC Antibody

  • Overview
  • Humanized Anti-TFPI IgG4-kappa antibody, Concizumab
  • Generic name
  • Concizumab

 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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