Mal-Phe-C4-Val-Cit-PAB-DMEA Catalog number: BADC-01278

Mal-Phe-C4-Val-Cit-PAB-DMEA is a sophisticated bioconjugate reagent used primarily in the development of targeted drug delivery systems, such as antibody-drug conjugates (ADCs) and peptide-drug conjugates (PDCs). The maleimide (Mal) group facilitates specific and efficient conjugation to thiol-containing molecules, such as antibodies or peptides. The Val-Cit (valine-citrulline) sequence functions as a cleavable linker, enabling controlled release of the drug payload in the tumor microenvironment through enzymatic cleavage. The PAB (p-aminobenzyl) group acts as a spacer, improving the overall stability and solubility of the conjugate. The DMEA (dimethylaminoethyl) moiety provides additional solubility and enhances the pharmacokinetics, ensuring prolonged circulation and reduced non-specific binding.

A major application of Mal-Phe-C4-Val-Cit-PAB-DMEA is in the design and development of targeted antibody-drug conjugates (ADCs) for cancer therapy. The compound allows for the covalent attachment of cytotoxic drugs to monoclonal antibodies or targeting peptides. The cleavable linker (Val-Cit) ensures that the payload is released only within the tumor cells, where specific enzymes cleave the linker, triggering the release of the cytotoxic drug. This targeted delivery system reduces the toxic side effects associated with conventional chemotherapy, as the drug is delivered specifically to cancerous tissues, thereby enhancing the therapeutic efficacy. The PEG-based linker and DMEA group further optimize the solubility and stability of the ADC, improving its pharmacokinetic profile.

Mal-Phe-C4-Val-Cit-PAB-DMEA is also widely employed in peptide-drug conjugates (PDCs), offering a tailored approach to targeted cancer therapy. By linking therapeutic agents to targeting peptides, this compound enables specific delivery of the drug to tumor cells. The cleavable Val-Cit linker ensures that the drug is released once the conjugate reaches its target, further enhancing the precision and effectiveness of the therapy. The addition of the DMEA group provides increased solubility and stability in the bloodstream, making the conjugate more efficient in reaching and acting on the target tissue. This makes Mal-Phe-C4-Val-Cit-PAB-DMEA highly effective in personalized cancer treatments, where peptide-based targeting agents play a crucial role in selective drug delivery.

In addition to drug delivery, Mal-Phe-C4-Val-Cit-PAB-DMEA is useful in molecular imaging and diagnostic applications. By attaching imaging agents such as fluorophores or radiolabels to antibodies or peptides, the compound allows for the targeted detection of biomarkers associated with cancer and other diseases. The cleavable Val-Cit linker ensures that the imaging agent is released in the target area, enhancing the accuracy and sensitivity of diagnostic imaging. The solubility-enhancing DMEA group ensures that the conjugate remains stable and effective in vivo, allowing for prolonged detection of disease markers. This application is key in the development of advanced diagnostic tools for precision medicine.