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910619

Sigma-Aldrich

Pomalidomide-PEG6-butyl alkyne

≥95%

Sinonimo/i:

N-(2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)-3,6,9,12,15,18-hexaoxahexacos-25-ynamide, Crosslinker–E3 Ligase ligand conjugate, Pomalidomide conjugate, Pomalidomide-2-2-2-2-2-2-6-alkyne, Protein degrader building block for PROTAC® research, Template for synthesis of targeted protein degrader

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About This Item

Formula empirica (notazione di Hill):
C33H45N3O11
Peso molecolare:
659.72
Codice UNSPSC:
51171641

ligand

pomalidomide

Saggio

≥95%

Stato

(Liquid or Semi-solid or Paste or Solid)

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(COCCOCCOCCOCCOCCOCCCCCCC#C)=O)=O)NC1=O

Applicazioni

Protein degrader builiding block Pomalidomide-PEG6-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.

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

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Codice della classe di stoccaggio

13 - Non 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
MKCL1561

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

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

Global Trade Item Number

SKUGTIN
910619-50MG

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