2,5-Pyrrolidinedione, 1-[(6-azido-1-oxohexyl)oxy]-

Description

Azido-Aca-NHS has an azide and NHS ester end group. The azide can undergo copper-catalyzed Click Chemistry reactions with alkynes, DBCO and BCN. The NHS ester can react with amine groups to form stable amide bonds.

Uses

N3-C5-NHS ester is a noncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). N3-C5-NHS ester is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

IC 50

Non-cleavable Linker

References

[1] Pyrrolobenzodiazepine Dimer Antibody-Drug Conjugates: Synthesis and Evaluation of Noncleavable Drug-Linkers. J Med Chem. 2017 Dec 14;60(23):9490-9507. DOI:10.1021/acs.jmedchem.7b00736