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Anti-TFPI (Concizumab)-MC-MMAF ADC (ADC-W-1792)

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

 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 (maleimidocaproyl)
  • Description
  • Noncleavable linkers, is considered noncleavable-meaning linker cleavage, and payload release does not depend on the differential properties between the plasma and some cytoplasmic compartments. Instead, the release of the cytotoxic drug is postulated to occur after internalization of the ADC via antigen-mediated endocytosis and delivery to lysosomal compartment, where the antibody is degraded to the level of amino acids through intracellular proteolytic degradation.

 ADC payload drug

  • Name
  • MMAF
  • 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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