Azido-PEG8-TFP ester
CAS No.: 1818294-49-3
Cat No.: BP-501513
4.5 
Azido-PEG8-TFP ester is a heterobifunctional polyethylene glycol linker that combines an azide handle with a tetrafluorophenyl (TFP) ester, enabling orthogonal conjugation in PROTAC workflows. Structurally, it features an eight-unit PEG chain that provides aqueous solubility and spatial flexibility, a terminal azide group suitable for strain-promoted or copper-catalyzed azide–alkyne cycloaddition, and a reactive TFP ester that forms stable amide bonds with primary amines on targeting ligands or other PROTAC components. In targeted protein degradation design, this linker mediates controlled attachment between a ligand-bearing amine (e.g., for installation of the PEG spacer) and a second module introduced via azide–click chemistry, allowing tuning of linker length and geometry to optimize ternary complex formation. Its value lies in improving conjugation efficiency and experimental modularity, supporting systematic structure–activity studies in PROTAC synthesis and characterization.
Structure of 1818294-49-3
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Azido-PEG8-TFP ester is a bifunctional PROTAC linker designed to connect a targeting ligand bearing an amine-reactive handle with an azide-bearing partner for subsequent conjugation. Its PEG-based spacer improves solubility and provides conformational flexibility, while the TFP ester enables efficient acyl transfer to nucleophilic residues. This combination supports modular PROTAC assembly and optimization, and the following points describe its structure and practical reactivity considerations in detail.
Structure: The linker contains a poly(ethylene glycol) chain terminated by an azide group and a trifluoromethyl-substituted TFP ester. It features an azide functionality for bioorthogonal coupling and an activated carboxylate for acylation. The ether-rich PEG backbone imparts hydrophilicity and chain flexibility.
Reactivity: The TFP ester typically reacts with primary amines under mild, nucleophilic acyl-substitution conditions, forming stable amide bonds. The azide group is compatible with copper-catalyzed or strain-promoted azide–alkyne cycloaddition strategies for modular attachment to complementary partners. Commonly used solvents include polar aprotic media or aqueous buffers with controlled pH, while catalysts for click chemistry are selected to match the chosen azide coupling format.
* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2
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