Azido-PEG1-amine
Azido-PEG1-amine is a short polyethylene glycol linker bearing a terminal azide and a primary amine, enabling versatile bioconjugation in PROTAC and targeted protein degradation workflows. Structurally, the PEG segment provides a flexible, hydrophilic spacer that can reduce steric interference between the two PROTAC arms, while the azide group serves as a handle for copper-free or copper-catalyzed azide–alkyne cycloaddition (“click”) to install or exchange the E3 ligase or warhead moiety. The terminal amine provides an orthogonal functional group for amide coupling, reductive amination, or salt formation, facilitating controlled attachment to activated carboxylic acids or activated esters. In PROTAC design, this dual-reactive chemistry supports modular synthesis, allowing researchers to rapidly generate linker variants and optimize spatial arrangement for productive ternary complex formation. Its small, flexible PEG length is particularly useful when minimal linker extension is desired to preserve binding affinity and maintain degradation potency.
Structure of 464190-91-8
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Azido-PEG1-amine is a polyethylene glycol (PEG)-based bifunctional linker designed for modular construction of PROTACs via orthogonal functional group chemistry. Its azide handle enables reliable conjugation through widely used click-type reactions, while the terminal amine supports complementary coupling strategies. The flexible PEG spacer can help tune solubility and presentation of ligands to the recruited target and E3 ligase, supporting efficient ternary complex formation. Detailed structural and reactivity considerations are provided below.
Structure: Azido-PEG1-amine contains an azide functional group and a terminal primary amine connected through a short PEG chain. It features ether linkages within the PEG segment and a carbon–nitrogen bond at the amine, providing conformational flexibility and polarity that promote aqueous compatibility.
Reactivity: The azide group is well suited for copper-catalyzed azide–alkyne cycloaddition or related azide-based conjugation approaches under conditions compatible with biomolecule-linked partners. The terminal amine can participate in amide-bond formation or other amine-selective coupling chemistries using activated carboxylic acids or electrophilic derivatives. Typical workflows use polar organic solvents and standard coupling bases, with reaction design guided by maintaining linker stability and preserving ligand integrity.
* 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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