Val-Ala-PAB-OH is a cleavable ADC linker with a terminal hydroxyl group. The Val-Ala is effectively cleaved by lysosomal proteolytic enzymes while being highly stable in human plasma, making this a potentent stragy in ADC linker design. The hydroxyl group enables further derivatization or replacement with other reactive functional groups.
Val-Ala-PAB is a building block in the synthesis of Tesirine (a.k.a. SG3249), a clinical antibody-drug conjugate pyrrolobenzodiazepine dimer payload. Reagent in the preparation of pyrrolobenzodiazepine dimers and their antibody conjugates containing peptide linkers useful for treating proliferative including cancer.
