This ADC product is comprised of an anti-CD40 monoclonal antibody conjugated via a MC-Vc-PAB linker to SN38. The SN-38 is targeted to certain cancers by immunerecognition and delivered into cancer cells via receptor mediated endocytosis. Within the cell, SN-38 binds to DNA, causes DNA damage.
ADC Target
- Alternative Names
- CD40; CD40 molecule, TNF receptor superfamily member 5; TNFRSF5, tumor necrosis factor receptor superfamily, member 5; tumor necrosis factor receptor superfamily member 5; Bp50; p50; CD40L receptor; CD40 type II isoform; B cell-associated molecule; B cellMaytenus 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.
- Target Entrez Gene ID
- 958
- Overview
- This gene is a member of the TNF-receptor superfamily. The encoded protein is a receptor on antigen-presenting cells of the immune system and is essential for mediating a broad variety of immune and inflammatory responses including T cell-dependent immunoglobulin class switching, memory B cell development, and germinal center formation. AT-hook transcription factor AKNA is reported to coordinately regulate the expression of this receptor and its ligand, which may be important for homotypic cell interactions. Adaptor protein TNFR2 interacts with this receptor and serves as a mediator of the signal transduction. The interaction of this receptor and its ligand is found to be necessary for amyloid-beta-induced microglial activation, and thus is thought to be an early event in Alzheimer disease pathogenesis. Mutations affecting this gene are the cause of autosomal recessive hyper-IgM immunodeficiency type 3 (HIGM3). Multiple alternatively spliced transcript variants of this gene encoding distinct isoforms have been reported.
ADC Antibody
- Overview
- Humanized Anti-CD40 IgG1 antibody, Dacetuzumab
ADC Linker
- Name
- MC-Vc-PAB (maleimidocaproyl-valine-citrulline-p-aminobenzoyloxycarbonyl)
- Description
- Peptide linkers, belonging to Enzymatically cleavable linkers, combine greater systemic stability with rapid enzymatic release of the drug in the target cell. The scission of peptidic bonds relies on lysosomal proteolytic enzymes, which have very low activities in blood due to endogenous inhibitors and the unfavorably high pH value of blood.
ADC payload drug
- Name
- SN-38 (7-ethyl-10-hydroxycamptothecin)
- Description
- SN38 (7-ethyl-10-hydroxy camptothecin) is an active metabolite of the cancer prodrug, irinotecan, with the ability of inhibiting Topoisomerase I, which is belong to the camptothecin family. SN-38 is formed via hydrolysis of irinotecan by carboxylesterases and metabolized via glucuronidation by UGT1A1.
For Research Use Only. NOT FOR CLINICAL USE.
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