Anti-CSF1R (Emactuzumab)-MC-Vc-PAB-DMEA-(PEG2)-duocarmycin SA ADC (ADC-W-2455)

This ADC product is comprised of an anti-CSF1R 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
  • 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-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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