This ADC product is comprised of an anti-TNFSF4 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
- TNFSF4; tumor necrosis factor (ligand) superfamily, member 4; tax transcriptionally activated glycoprotein 1, 34kD , TXGP1; tumor necrosis factor ligand superfamily member 4; CD252; gp34; OX 40L; OX40L; CD134 ligand; glycoprotein Gp34; OX40 antigen ligand; TAX transcriptionally-activated glycoprotein 1; tax-transcriptionally activated glycoprotein 1 (34kD); GP34; OX4OL; TXGP1; CD134L; OX-40L;
- Target Entrez Gene ID
- 7292
- Overview
- This gene encodes a cytokine of the tumor necrosis factor (TNF) ligand family. The encoded protein functions in T cell antigen-presenting cell (APC) interactions and mediates adhesion of activated T cells to endothelial cells. Polymorphisms in this gene have been associated with Sjogren's syndrome and systemic lupus erythematosus. Alternative splicing results in multiple transcript variants.
ADC Antibody
- Overview
- Human Anti-TNFRSF4 IgG1-kappa antibody, Oxelumab
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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