Alkyne-PEG4-phosphoramidite
CAS No.: 1682657-14-2
Cat No.: BP-501044
Purity: >95%
4.5 
Alkyne-PEG4-phosphoramidite is a PEG-based, linker building block designed for assembling PROTACs and other targeted protein degradation conjugates via oligonucleotide-style phosphoramidite chemistry. Structurally, it contains a terminal alkyne handle for subsequent click-type conjugation and a short, flexible tetraethylene glycol (PEG4) spacer that increases solubility and reduces steric interference between the two functional domains. The phosphoramidite functionality enables controlled incorporation into synthetic linker scaffolds, allowing researchers to position the alkyne at a defined distance from the attachment point. In PROTAC design, this kind of spacer-and-handle architecture supports efficient coupling of the E3 ligase ligand and the target-binding ligand (or other modules) while maintaining productive geometry for ternary-complex formation. As a modular intermediate, it is valuable for rapid structure–activity optimization, particularly when tuning linker length and flexibility to improve degradation potency and cellular activity.
Structure of 1682657-14-2
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Alkyne-PEG4-phosphoramidite is a PEG-based linker designed for modular PROTAC assembly, enabling efficient coupling of alkyne-functional components under phosphoramidite chemistry. Its flexible polyethylene glycol segment supports productive spatial presentation of ligands, while the alkyne handle facilitates downstream conjugation strategies commonly used in targeted protein degradation workflows. The features and practical synthetic considerations of this linker are described in detail below.
Structure: The linker contains a polyethylene glycol chain providing conformational flexibility and enhanced solubility, terminating in an alkyne functionality and a phosphoramidite reactive center. It incorporates P–N and P–O connectivity typical of phosphoramidites, with ether linkages along the PEG backbone.
Reactivity: Phosphoramidite groups are typically activated by mild Lewis acids to form reactive intermediates that couple with alcohol or other nucleophiles, enabling controlled bond formation under anhydrous conditions. For PROTAC construction, the alkyne functionality can be preserved for orthogonal post-coupling reactions, while the PEG segment supports stable conjugate formation. Common approaches use dry polar solvents and standard phosphoramidite activation/coupling protocols with appropriate base and inert atmosphere handling.
* 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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