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Anti-CSF1R (Emactuzumab)-MC-MMAF ADC (ADC-W-2452)

This ADC product is comprised of an anti-CSF1R 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
  • CSF1R
  • Alternative Names
  • CSF1R; colony stimulating factor 1 receptor; FMS, McDonough feline sarcoma viral (v fms) oncogene homolog; macrophage colony-stimulating factor 1 receptor; C FMS; CD115; CSFR; CSF-1-R; CD115 antigen; CSF-1 receptor; FMS proto-oncogene; proto-oncogene c-Fms; macrophage colony stimulating factor I receptor; McDonough feline sarcoma viral (v-fms) oncogene homolog; FMS; FIM2; HDLS; C-FMS; CSF-1R; M-CSF-R;
  • Target Entrez Gene ID
  • 1436
  • Overview
  • The protein encoded by this gene is the receptor for colony stimulating factor 1, a cytokine which controls the production, differentiation, and function of macrophages. This receptor mediates most if not all of the biological effects of this cytokine. Ligand binding activates the receptor kinase through a process of oligomerization and transphosphorylation. The encoded protein is a tyrosine kinase transmembrane receptor and member of the CSF1/PDGF receptor family of tyrosine-protein kinases. Mutations in this gene have been associated with a predisposition to myeloid malignancy. The first intron of this gene contains a transcriptionally inactive ribosomal protein L7 processed pseudogene oriented in the opposite direction. Alternative splicing results in multiple transcript variants. Expression of a splice variant from an LTR promoter has been found in Hodgkin lymphoma (HL), HL cell lines and anaplastic large cell lymphoma.

 ADC Antibody

  • Overview
  • Humanized Anti-CSF1R IgG1-kappa antibody, Emactuzumab
  • Generic name
  • Emactuzumab

 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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