This ADC product is comprised of an anti-ITGAV+ITGB3 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
- ITGAV+ITGB3
- Overview
- Integrins are integral cell-surface proteins composed of an alpha chain and a beta chain. They are known to participate in cell adhesion as well as cell-surface mediated signalling. Integrins are heterodimeric integral membrane proteins composed of an alpha chain and a beta chain. CD51 encodes integrin alpha chain V. The I-domain containing integrin alpha V undergoes post-translational cleavage to yield disulfide-linked heavy and light chains, that combine with multiple integrin beta chains to form different integrins. Alpha-V integrins have been implicated in many developmental processes and are therapeutic targets for inhibition of angiogenesis and osteoporosis.
ADC Antibody
- Overview
- Humanized Anti-ITGAV+ITGB3 IgG1 antibody, Etaracizumab
- Generic name
- Etaracizumab
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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