FMoc-NH-5(ethylene glycol)-acetic acid

Product NameFMoc-NH-5(ethylene glycol)-acetic acid
CAS635287-26-2
MFC27H35NO9
MW517.57
EINECS
MOL File635287-26-2.mol

Chemical Properties

Boiling point	704.3±60.0 °C(Predicted)
Density	1.224±0.06 g/cm3(Predicted)
storage temp.	2-8°C
pka	3.39±0.10(Predicted)
form	Viscous Liquid
color	Colorless to light yellow

Usage And Synthesis

Description

Fmoc-NH-PEG5-CH2COOH is a PEG linker containing an Fmoc-protected amine and a terminal carboxylic acid. The hydrophilic PEG spacer increases solubility in aqueous media. The Fmoc group can be deprotected under basic condition to obtain the free amine which can be used for further conjugations. 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.

Biological Activity

Fmoc-NH-PEG5-CH2COOH is a degradable ADC linker for antibody drug conjugate (ADC) synthesis. It is also a PEG-based PROTAC linker, which can be used for PROTAC synthesis.

in vitro

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.

target

Cleavable

Alkyl/ether

PEGs