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901496

Sigma-Aldrich

Pomalidomide-C6-CO2H

≥98%

Synonym(e):

7-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)heptanoic acid, 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

Empirische Formel (Hill-System):
C20H23N3O6
CAS-Nummer:
2225940-50-9
Molekulargewicht:
401.41
UNSPSC-Code:
12352101
NACRES:
NA.22

ligand

pomalidomide

Qualitätsniveau

100

Assay

≥98%

Form

powder or crystals

Eignung der Reaktion

reactivity: amine reactive
reagent type: ligand-linker conjugate

Funktionelle Gruppe

carboxylic acid

Lagertemp.

2-8°C

SMILES String

O=C1N(C2CCC(NC2=O)=O)C(C3=C1C=CC=C3NCCCCCCC(O)=O)=O

Anwendung

Protein degrader builiding block Pomalidomide-C6-CO2H enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand and an alkyl-chain crosslinker with pendant carboxylic acid for reactivity with an amine 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 carboxyl group, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

Sonstige Hinweise

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

Rechtliche Hinweise

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

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Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

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Flammpunkt (°C)

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Analysenzertifikate (COA)

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Die Dokumentenbibliothek aufrufen

Momar Toure et al.
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Daniel P Bondeson et al.
Annual review of pharmacology and toxicology, 57, 107-123 (2016-10-13)
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Artikel

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.

Partial PROTACs 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.

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