Anti-CTLA4 (Ipilimumab)-MC-Vc-PAB-DMEA-(PEG2)-duocarmycin SA ADC (ADC-W-1003)

This ADC product is comprised of an anti-CTLA4 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
  • CTLA4
  • Alternative Names
  • CTLA4; cytotoxic T-lymphocyte-associated protein 4; celiac disease 3 , CELIAC3; cytotoxic T-lymphocyte protein 4; CD; CD28; CD152; GSE; ICOS; CD152 isoform; celiac disease 3; cytotoxic T-lymphocyte antigen 4; cytotoxic T-lymphocyte-associated antigen 4; cMaytenus ovatus. Maytansinoids can bind to tubulin at or near the vinblastine-binding site, which interfere the formation of microtubules and depolymerize already formed microtubules, inducing mitotic arrest in the intoxicat
  • Target Entrez Gene ID
  • 1493
  • Overview
  • This gene is a member of the immunoglobulin superfamily and encodes a protein which transmits an inhibitory signal to T cells. The protein contains a V domain, a transmembrane domain, and a cytoplasmic tail. Alternate transcriptional splice variants, encoding different isoforms, have been characterized. The membrane-bound isoform functions as a homodimer interconnected by a disulfide bond, while the soluble isoform functions as a monomer. Mutations in this gene have been associated with insulin-dependent diabetes mellitus, Graves disease, Hashimoto thyroiditis, celiac disease, systemic lupus erythematosus, thyroid-associated orbitopathy, and other autoimmune diseases.

 ADC Antibody

  • Overview
  • Human Anti-CTLA4 IgG1-kappa antibody, Ipilimumab
  • Generic name
  • Ipilimumab
  • Host animal
  • Human
  • Species Reactivity
  • Human

 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.

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