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910503

Sigma-Aldrich

Pomalidomide-PEG2-butyl alkyne

≥95%

Sinónimos:

N-(2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)-2-(2-(oct-7-yn-1-yloxy)ethoxy)acetamide, Crosslinker−E3 Ligase ligand conjugate, Pomalidomide conjugate, Pomalidomide-2-2-6-alkyne, Protein degrader building block for PROTAC® research, Template for synthesis of targeted protein degrader

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About This Item

Fórmula empírica (notación de Hill):
C25H29N3O7
Peso molecular:
483.51
Código UNSPSC:
51171641

ligand

pomalidomide

Análisis

≥95%

formulario

(Liquid or Semi-Solid or Paste or Solid)

idoneidad de la reacción

reaction type: click chemistry
reagent type: ligand-linker conjugate

grupo funcional

alkyne

temp. de almacenamiento

2-8°C

cadena SMILES

O=C(C(CC1)N(C2=O)C(C3=C2C=CC=C3NC(COCCOCCCCCCC#C)=O)=O)NC1=O

Aplicación

Protein degrader builiding block Pomalidomide-PEG2-butyl alkyne enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand, a linker with both hydrophobic and hydrophilic moieties, and a pendant alkyne for click chemistry with an azide on the target ligand. Because even slight alterations in ligands and crosslinkers can affect ternary complex formation between the target, E3 ligase, and PROTAC, many analogs are prepared to screen for optimal target degradation. When used with other protein degrader building blocks with a pendant alkyne, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

Otras notas

Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation

Portal: Building PROTAC® Degraders for Targeted Protein Degradation

Targeted Protein Degradation by Small Molecules

Small-Molecule PROTACS: New Approaches to Protein Degradation

Targeted Protein Degradation: from Chemical Biology to Drug Discovery

Impact of linker length on the activity of PROTACs

Información legal

PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license

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Código de clase de almacenamiento

13 - Non Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable

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Certificados de análisis (COA)

Lot/Batch Number
MKCL0803

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Momar Toure et al.
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The current inhibitor-based approach to therapeutics has inherent limitations owing to its occupancy-based model: 1) there is a need to maintain high systemic exposure to ensure sufficient in vivo inhibition, 2) high in vivo concentrations bring potential for off-target side effects, and 3) there is
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Artículos

Degrader Building Blocks for Targeted Protein Degradation

Partial PROTACs are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

Degrader Building Blocks for Targeted Protein Degradation

Protein Degrader Building Blocks are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

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