N3-PEG-Ala-Ala-Asn-PAB-OH

Azido-functionalized discrete poly(ethylene glycol)-alanyl-alanyl-asparagine-p-aminobenzyl alcohol (N3-PEG-Ala-Ala-Asn-PAB-OH) is an ADC linker intermediate containing a defined-length PEG spacer. It contains an azide reactive terminus and an alanine–alanine–asparagine tripeptide. Discrete chain lengths with different degrees of polymerization are available. The azide can undergo copper-catalyzed click reactions with terminal alkynes or copper-free click conjugation with strained alkynes such as DBCO and BCN. The alanine–alanine–asparagine tripeptide provides a sequence variable for studies of protease-cleavable linkers. The PAB spacer links peptide cleavage to the subsequent self-immolation process. The PAB hydroxyl group retains a synthetic handle for subsequent activation and payload derivatization.

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