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CAS No.: 644981-35-1; Val-Cit-PAB-MMAE. PROPERTIES: Val-Cit-PAB-MMAE is a synthetic linker-drug conjugate with molecular weight approximately 1156.2 g/mol. This compound features a valine-citrulline dipeptide linker connected via p-aminobenzyloxycarbonyl (PAB) group to monomethyl auristatin E (MMAE). It has limited aqueous solubility, generally requiring dimethyl sulfoxide (DMSO) concentrations above 10 mg/mL for dissolution. Storage recommendations include frozen conditions at -20 C in screw-capped vials, protected from light and moisture. Safety considerations involve stringent handling protocols due to its cytotoxic nature; engineering controls and chemical fume hoods are mandatory during manipulation. APPLICATIONS: As an integral component in antibody-drug conjugates (ADCs), Val-Cit-PAB-MMAE enables targeted cancer therapy. The dipeptide linker is designed for proteolytic cleavage by cathepsin B in tumor cells, releasing cytotoxic MMAE. This technology has been utilized in developing several anticancer biologics, including those targeting CD30-positive malignancies as described in Nature Biotechnology preclinical studies. Its application extends to creating ADCs against various cancer antigens, with research in Molecular Cancer Therapeutics demonstrating effective tumor growth inhibition in xenograft models. Additionally, Val-Cit-PAB-MMAE serves as a research tool for studying intracellular drug release mechanisms and linker stability in ADC development pipelines, with methodological details published in Bioconjugate Chemistry analytical reports.