Azido-PEG1-C2-methylamine
Azido-PEG1-C2-methylamine is a short, bifunctional polyethylene glycol (PEG) linker bearing a terminal azide group and a C2 methylamine functionality. Structurally, it provides a flexible, hydrophilic spacer that can be used to connect two PROTAC-related fragments while maintaining appropriate spatial separation for productive ternary-complex formation. The azide handle enables bioorthogonal conjugation via copper-catalyzed or strain-promoted azide–alkyne cycloaddition, allowing researchers to attach the linker to an alkyne-bearing ligand (e.g., E3 ligase binder or target-binding moiety) under conditions compatible with many organic scaffolds. The methylamine group offers a reactive primary amine for subsequent coupling strategies such as amide-bond formation or reductive amination, facilitating modular assembly of degraders. In targeted protein degradation workflows, this linker is useful for tuning linker length, polarity, and attachment geometry, which can materially influence binding orientation, cellular uptake, and overall degradation potency.
Structure of 1835759-88-0
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Azido-PEG1-C2-methylamine is a PEG-based bifunctional linker designed for modular assembly of PROTACs, enabling efficient conjugation between a targeting ligand and an E3-recruiting moiety. Its azide handle supports widely used chemoselective coupling strategies, while the PEG spacer improves solubility and can help tune linker flexibility and effective intramolecular reach. The following sections describe its structure and practical reactivity considerations for PROTAC construction.
Structure: The molecule contains an azide functional group attached to a short polyethylene glycol segment, terminating in a methylamine. It features ether linkages within the PEG chain, with an amine suitable for nucleophilic derivatization. The combination supports polar, water-compatible behavior and robust chemical handle diversity.
Reactivity: The azide group is commonly used in copper-catalyzed azide–alkyne cycloaddition or related azide-based conjugations, proceeding via formation of a reactive copper–acetylide intermediate under standard conditions. The methylamine enables amide or urea formation through nucleophilic acyl substitution using activated carboxylic acid derivatives. Typical workflows employ polar aprotic solvents and standard base/activator systems compatible with PROTAC ligand stability.
* 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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