Azido-PEG4-Val-Cit-PAB-OH

Description

Azido-PEG4-Val-Cit-PAB-OH is a cleavable peptide linker. The Val-Cit will specifically be cleaved by Cathepsin B. Azido group enable click chemistry with DBCO, BCN or other Alkyne group. PEG spacer increases aqueous solubility.

Uses

Azido-PEG4-Val-Cit-PAB-OH is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. Azido-PEG4-Val-Cit-PAB-OH is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[2]. Azido-PEG4-Val-Cit-PAB-OH 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

Protease Cleavable Linker; PEGs; Cleavable Linker

References

[1] Dan N, et al. Antibody-Drug Conjugates for Cancer Therapy: Chemistry to Clinical Implications. Pharmaceuticals (Basel). 2018 Apr 9;11(2). pii: E32. DOI:10.3390/ph11020032
[2] An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562. DOI:10.1016/j.ebiom.2018.09.005