This ADC product is comprised of an anti-TNC 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
- Alternative Names
- TNC; tenascin C; hexabrachion (tenascin C, cytotactin) , HXB; tenascin; hexabrachion (tenascin); MGC167029; TN; GP 150-225; cytotactin; neuronectin; myotendinous antigen; tenascin-C isoform 14/AD1/16; glioma-associated-extracellular matrix antigen; GP; JI; HXB; GMEM; TN-C; 150-225;
- Target Entrez Gene ID
- 3371
- Overview
- This gene encodes an extracellular matrix protein with a spatially and temporally restricted tissue distribution. This protein is homohexameric with disulfide-linked subunits, and contains multiple EGF-like and fibronectin type-III domains. It is implicated in guidance of migrating neurons as well as axons during development, synaptic plasticity, and neuronal regeneration.
ADC Antibody
- Overview
- Human Anti-TNC IgG2b antibody, Tenatumomab
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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