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Anti-KDR (Ramucirumab)-SMCC-DM1 ADC (ADC-W-1514)

This ADC product is comprised of an anti-KDR monoclonal antibody conjugated via a SMCC linker to DM1. The DM1 is targeted to certain cancers by immunerecognition and delivered into cancer cells via receptor mediated endocytosis. Within the cell, DM1 binds to tubulins, interrupts microtubule dynamics, and subsequently, induces cell death.

 ADC Target

  • Name
  • KDR
  • Alternative Names
  • KDR; kinase insert domain receptor (a type III receptor tyrosine kinase); vascular endothelial growth factor receptor 2; CD309; FLK1; VEGFR; VEGFR2; soluble VEGFR2; fetal liver kinase 1; fetal liver kinase-1; protein-tyrosine kinase receptor Flk-1; tyrosine kinase growth factor receptor;
  • Target Entrez Gene ID
  • 3791
  • Overview
  • Vascular endothelial growth factor (VEGF) is a major growth factor for endothelial cells. This gene encodes one of the two receptors of the VEGF. This receptor, known as kinase insert domain receptor, is a type III receptor tyrosine kinase. It functions as the main mediator of VEGF-induced endothelial proliferation, survival, migration, tubular morphogenesis and sprouting. The signalling and trafficking of this receptor are regulated by multiple factors, including Rab GTPase, P2Y purine nucleotide receptor, integrin alphaVbeta3, T-cell protein tyrosine phosphatase, etc.. Mutations of this gene are implicated in infantile capillary hemangiomas.

 ADC Antibody

  • Overview
  • Human Anti-KDR IgG1-kappa antibody, Ramucirumab
  • Generic name
  • Ramucirumab
  • Host animal
  • Human

 ADC Linker

  • Name
  • SMCC (N-succinimidyl 4-(Nmaleimidomethyl)cyclohexane-1-carboxylate)
  • Description
  • Disulfide Linkers, are extensively exploited as a chemically labile linkage. Since the release of disulfide-linked drugs requires a cytoplasmic thiol cofactor, such as glutathione (GSH). Disulfides maintain stable at physiological pH and only when ADCs are internalized inside cells, the cytosol provides reducing environment including intracellular enzyme protein disulfide isomerase, or similar enzymes, drugs can be released.

 ADC payload drug

  • Name
  • DM1 (N2'-Deacetyl-N2'-(3-mercapto-1-oxopropyl)maytansine)
  • Description
  • Derived from Maytansinoid,a group of cytotoxins structurally similar to rifamycin, geldanamycin, and ansatrienin. The eponymous natural cytotoxic agent maytansine is a 19-member lactam (ansa macrolide) structure originally isolated from the Ethiopian shrub Maytenus 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 intoxicated cells.

For Research Use Only. NOT FOR CLINICAL USE.

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