DBCO-Val-Cit-PAB-PNP is a cleavable linker used in the synthesis of antibody-drug conjugates (ADCs). It comprises a dibenzocyclooctyne moiety, a valine-citrulline (Val-Cit) dipeptide, a para-aminobenzyl (PAB) spacer, and a p-nitrophenyl (PNP) ester.
Key Features:
- DBCO Moiety: Enables strain-promoted azide-alkyne cycloaddition (SPAAC) for copper-free click chemistry with azide-containing molecules.
- Val-Cit Dipeptide: Serves as a protease-cleavable linker, specifically cleaved by cathepsin B, facilitating controlled drug release within target cells.
- PAB Spacer: Acts as a self-immolative linker, ensuring efficient payload release upon cleavage.
- PNP Ester: Functions as a leaving group, allowing conjugation with amine-containing payloads.
Applications:
- Antibody-Drug Conjugates (ADCs): Facilitates the attachment of cytotoxic drugs to antibodies, enabling targeted cancer therapy.
- Bioconjugation: Supports the development of targeted therapeutics through efficient coupling with azide-functionalized molecules.
- Drug Delivery Research: Assists in creating prodrugs that release active agents in response to specific enzymatic activity within target cells.
Handling and Storage:
- Storage Conditions: Store at -20°C in a dry, light-protected environment.
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