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901834

Sigma-Aldrich

Pomalidomide-PEG5-Alkyne

≥95%

Sinonimo/i:

N-(2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)-4,7,10,13,16-pentaoxanonadec-18-ynamide, Crosslinker−E3 Ligase ligand conjugate, Protein degrader building block for PROTAC® research, Template for synthesis of targeted protein degrader

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About This Item

Formula empirica (notazione di Hill):
C27H33N3O10
Peso molecolare:
559.57
Codice UNSPSC:
51171641
NACRES:
NA.22

ligand

pomalidomide

Saggio

≥95%

Forma fisica

powder or crystals

Impiego in reazioni chimiche

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

Gruppo funzionale

alkyne

Temperatura di conservazione

2-8°C

Stringa SMILE

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

Categorie correlate

Applicazioni

Protein degrader builiding block Pomalidomide-PEG5-Alkyne enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand and a PEGylated crosslinker with 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 group, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

Automate your CRBN-PEG based PROTACs with Synple Automated Synthesis Platform (SYNPLE-SC002)

Altre note

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

Note legali

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

Prodotti correlati

N° Catalogo
Descrizione
Determinazione del prezzo

P0018

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(S,R,S)-AHPC-PEG3-NH2 hydrochloride, ≥95%

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(S,R,S)-AHPC-PEG2-Alkyne, ≥95%

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Pomalidomide-PEG1-NH2 hydrochloride, ≥95%

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Pomalidomide-PEG2-Alkyne, ≥95%

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(S,R,S)-AHPC-PEG4-Alkyne

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(S,R,S)-AHPC-PEG3-azide, ≥95%

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Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

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Certificati d'analisi (COA)

Lot/Batch Number
MKCG7399

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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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