Overview | 15-azido -4,7,10,13-tetraoxopentanoic acid is an organic intermediate. It is reported in the literature that 15-azido -4,7,10,13-tetraoxopentanoic acid can be used to prepare suicide linkers. Suicide linkers can connect rosin-55 to monoclonal antibodies or conjugates made of peptides that are highly effective in anti-tumor cells. |
preparation | 15-azido -4,7,10,13-tetraoxo-tert-butyl acid (0.22g;0.63mmol) is dissolved in pure DCM (5mL) and TFA(5mL) is added. The solution was stirred at room temperature for 1.5 hours. Next, the volatile compounds are removed in a vacuum, the residue is dissolved in diethyl ether (10mL) and the solvent is evaporated (repeated twice). Concentrate the solution until dry. 15-azido -4,7,10,13-tetraoxopentenoic acid (0.18g;0.62mmol;98%) was obtained in the form of a colorless oil. |
biological activity | Azido-PEG4-C2-acid is a PEG-based PROTAC linker that can be used to synthesize vRucaparib-TP4. Azido-PEG4-C2-acid is also a non-cleavable ADC linker with 4-unit PEG, which can be used to synthesize antibody-coupled drugs (ADC). |
in vitro study | 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. ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker. |