Anti-ERBB2 (trastuzumab)-AcLys-Putrescinyl-Geldanamycin ADC (ADC-W-638)

This ADC product is comprised of an engineerd anti-ERBB2 antibody (trastuzumab with LLQGG tag at Fc) conjugated via a AcLys-Putrescinyl linker to Geldanamycin. The Geldanamycin is targeted to certain cancers by immunerecognition and delivered into cancer cells via receptor mediated endocytosis. Within the cell, Geldanamycin binds to Hsp90, induces cell death.

 ADC Target

  • Name
  • ERBB2
  • Alternative Names
  • ERBB2; erb-b2 receptor tyrosine kinase 2; NEU; NGL; HER2; TKR1; CD340; HER-2; MLN 19; HER-2/neu; receptor tyrosine-protein kinase erbB-2; herstatin; p185erbB2; proto-oncogene Neu; c-erb B2/neu protein; proto-oncogene c-ErbB-2; metastatic lymph node gene 1
  • Target Entrez Gene ID
  • 2064
  • Overview
  • This gene encodes a member of the epidermal growth factor (EGF) receptor family of receptor tyrosine kinases. This protein has no ligand binding domain of its own and therefore cannot bind growth factors. However, it does bind tightly to other ligand-bound EGF receptor family members to form a heterodimer, stabilizing ligand binding and enhancing kinase-mediated activation of downstream signalling pathways, such as those involving mitogen-activated protein kinase and phosphatidylinositol-3 kinase. Allelic variations at amino acid positions 654 and 655 of isoform a (positions 624 and 625 of isoform b) have been reported, with the most common allele, Ile654/Ile655, shown here. Amplification and/or overexpression of this gene has been reported in numerous cancers, including breast and ovarian tumors. Alternative splicing results in several additional transcript variants, some encoding different isoforms and others that have not been fully characterized.

 ADC Antibody

  • Overview
  • Engineerd Trastuzumab with LLQGG tag at Fc
  • Generic name
  • trastuzumab
  • Host animal
  • Mouse
  • Species Reactivity
  • Human

 ADC Linker

  • Name
  • AcLys-Putrescinyl

 ADC payload drug

  • Name
  • Geldanamycin
  • Description
  • Geldanamycin is a 1,4-benzoquinone ansamycin antitumor antibiotic that inhibits the function of Hsp90 (Heat Shock Protein 90) by binding to the unusual ADP/ATP-binding pocket of the protein. HSP90 client proteins play important roles in the regulation of the cell cycle, cell growth, cell survival, apoptosis, angiogenesis and oncogenesis.
    Hsp90-geldanamycin complex. PDB 1yet
    Geldanamycin induces the degradation of proteins that are mutated in tumor cells such as v-Src, Bcr-Abl and p53 preferentially over their normal cellular counterparts. This effect is mediated via HSP90. Despite its potent antitumor potential, geldanamycin presents several major drawbacks as a drug candidate such as hepatotoxicity, further, Jilani et al. reported that geldanamycin induces the apoptosis of erythrocytes under physiological concentrations.

For Research Use Only. NOT FOR CLINICAL USE.


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