Bromo-PEG2-azide
Bromo-PEG2-azide is a bifunctional polyethylene glycol linker featuring a terminal azide group for bioorthogonal conjugation and a terminal bromide handle for further chemical derivatization. The PEG2 chain provides a short, flexible hydrophilic spacer that can reduce steric interference between a PROTAC warhead and an E3-ligase ligand, while maintaining sufficient proximity for productive ternary-complex formation. In PROTAC construction, the azide functionality enables efficient attachment via azide-reactive chemistries (e.g., copper-free or copper-catalyzed azide–alkyne cycloaddition, depending on compatibility), allowing researchers to connect the linker to complementary partners under mild conditions. The bromide site can be used to introduce additional functional groups or to support alternative coupling strategies, facilitating modular assembly of degradation scaffolds. This linker is valuable for systematic structure–activity relationship studies, enabling rapid optimization of linker length, polarity, and attachment geometry to improve targeted protein degradation performance.
Structure of 530151-56-5
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* For research and manufacturing use only. Not for human or clinical use.
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Bromo-PEG2-azide is a bifunctional PEG-based linker designed for modular assembly of PROTACs, enabling efficient conjugation between a ligand bearing an azide handle and a complementary partner containing a suitable coupling group. Its ether-rich polyethylene glycol scaffold provides conformational flexibility and improved solubility, while the orthogonal reactive termini support stepwise synthesis. The detailed Structure and Reactivity considerations below describe how this linker’s functional groups can be leveraged for targeted protein degradation workflows.
Structure: Bromo-PEG2-azide contains a short polyethylene glycol chain featuring ether linkages that confer flexibility and hydrophilicity. It bears an azide functionality for click-type coupling and a bromo leaving group for substitution chemistry. The molecule is an organohalide–azide conjugate with polar, hydrogen-bond-accepting ether atoms.
Reactivity: The azide group is well suited for copper-catalyzed azide–alkyne cycloaddition to connect PROTAC fragments under mild conditions, typically using a compatible alkyne partner and standard Cu(I) generation strategies in aqueous or mixed solvents. The bromo terminus can undergo nucleophilic substitution with amines or other nucleophiles to install additional handles. Orthogonal reactivity enables sequential functionalization to build PROTAC architectures while minimizing cross-reactivity.
* 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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