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Mal-PEG4-PFP is a PEG-containing maleimide conjugation reagent designed for thiol-reactive coupling. The maleimide group provides a selective handle for sulfhydryl-containing molecules, while the opposite terminus and spacer determine how the reagent can be connected to a payload, linker intermediate, or additional functional module. The molecule incorporates peg4 spacer and provides pfp ester (amine-reactive) for amine-bearing payloads/handles; orientation can be reversed depending adc strategy on the opposite side. It can be used in stepwise conjugation workflows that combine thiol-maleimide coupling with an orthogonal second reaction, with reaction order selected to suit the stability and accessibility of each functional group.
Structure of 1415800-42-8
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Mal-PEG4-PFP is a versatile bioconjugation reagent that combines a maleimide (Mal) group, a polyethylene glycol (PEG4) spacer, and a pentafluorophenyl (PFP) ester. The maleimide group facilitates the selective conjugation to thiol-containing molecules, such as peptides, proteins, or antibodies, while the PEG4 spacer provides solubility, stability, and improved pharmacokinetics. The PFP ester group reacts with amines, enabling the attachment of a wide range of functional groups, including drugs, imaging agents, or other bioactive molecules. This compound is widely used in targeted drug delivery, protein labeling, and bioorthogonal chemistry applications.
One of the primary applications of Mal-PEG4-PFP is in the development of antibody-drug conjugates (ADCs) for cancer therapy. By linking cytotoxic drugs or therapeutic agents to antibodies through the maleimide group, this conjugate ensures selective targeting of tumor cells that express specific surface markers. The PEG4 spacer improves the pharmacokinetics of the conjugate, enhancing its solubility and circulation time, which is critical for effective tumor targeting. The PFP ester allows for further functionalization by attaching imaging agents or other therapeutic molecules using the reaction with amines. This targeted delivery enhances drug efficacy while minimizing systemic toxicity, providing a more effective treatment strategy for cancer patients.
Mal-PEG4-PFP is also widely used in protein and peptide labeling for research purposes. The PFP ester group reacts with primary amines on proteins, peptides, or other biomolecules, enabling the covalent attachment of various functional groups, such as fluorescent dyes, enzymes, or affinity tags. The PEG4 spacer ensures that the conjugated biomolecule remains soluble and stable, which is crucial for maintaining its bioactivity in solution. This application is particularly beneficial in proteomics, cell biology, and biomolecular interaction studies, where precise labeling and tracking of proteins or peptides are essential for understanding cellular mechanisms and protein functions.
Additionally, Mal-PEG4-PFP is utilized in the design of advanced drug delivery systems and bioorthogonal chemistry applications. The maleimide group enables the conjugation of drugs or targeting ligands to biomolecules, while the PFP ester group allows for the attachment of other agents through amine reaction. The PEG4 spacer improves the pharmacokinetics of the conjugate, ensuring better stability and controlled release of the therapeutic agent. The bioorthogonal reactivity of the PFP group also makes this compound ideal for use in click chemistry, where precise and selective conjugation reactions are critical for the development of multifunctional drug delivery systems or imaging agents. This versatility is particularly valuable in targeted therapy and diagnostic imaging.
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