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Anti-MST1R (Narnatumab)-SPDB-DM4 ADC (ADC-W-1599)

This ADC product is comprised of an anti-MST1R monoclonal antibody conjugated via a SPDB linker to DM4. The DM4 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
  • MST1R
  • Alternative Names
  • MST1R; macrophage stimulating 1 receptor (c-met-related tyrosine kinase); PTK8, PTK8 protein tyrosine kinase 8 , RON; macrophage-stimulating protein receptor; CD136; CDw136; p185-Ron; MSP receptor; RON variant E2E3; MST1R variant RON30; MST1R variant RON62; soluble RON variant 1; soluble RON variant 2; soluble RON variant 3; soluble RON variant 4; c-met-related tyrosine kinase; PTK8 protein tyrosine kinase 8; RON; PTK8;
  • Target Entrez Gene ID
  • 4486
  • Overview
  • This gene encodes a cell surface receptor for macrophage-stimulating protein (MSP) with tyrosine kinase activity. The mature form of this protein is a heterodimer of disulfide-linked alpha and beta subunits, generated by proteolytic cleavage of a single-chain precursor. The beta subunit undergoes tyrosine phosphorylation upon stimulation by MSP. This protein is expressed on the ciliated epithelia of the mucociliary transport apparatus of the lung, and together with MSP, thought to be involved in host defense. Alternative splicing generates multiple transcript variants encoding different isoforms that may undergo similar proteolytic processing.

 ADC Antibody

  • Overview
  • Human Anti-MST1R IgG1-kappa antibody, Narnatumab
  • Generic name
  • Narnatumab
  • Host animal
  • Human

 ADC Linker

  • Name
  • SPDB (N-succinimidyl-4-(2-pyridyldithio)butyrate)
  • 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
  • DM4 (N2'-Deacetyl-N2'-(4-mercapto-4-methyl-1-oxopentyl)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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