Description
Amino-PEG2-acid is a PEG reagent containing an amino group with a terminal carboxylic acid. The hydrophilic PEG spacer increases solubility in aqueous media. The amino group is reactive with carboxylic acids, activated NHS esters, carbonyls (ketone, aldehyde) etc. The terminal carboxylic acid can react with primary amine groups in the presence of activators (e.g. EDC, or HATU) to form a stable amide bond.
Uses
Amino-PEG2-C2-acid is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Amino-PEG2-C2-acid is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Biological Activity
Amino-PEG2-C2-acid is a cleavable 3-unit PEG ADClinker for the synthesis of antibody-drug conjugated Ck (ADC). It is also a PEG-based PROTAClinker that can be used for PROTAC synthesis.
in vivo
ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
IC 50
Cleavable Linker; PEGs
References
[1] Antibody drug conjugate, intermediate, preparation method, pharmaceutical composition and uses thereof. WO2016197946A1.
