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910449

Sigma-Aldrich

Pomalidomide-PEG2-butyl CO2H

≥95%

Synonym(e):

7-(2-(2-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-2-oxoethoxy)ethoxy)heptanoic acid, Crosslinker−E3 ligase ligand conjugate, Pomalidomide conjugate, Pomalidomide-2-2-6-acid, 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):
C24H29N3O9
Molekulargewicht:
503.50
UNSPSC-Code:
12352101
NACRES:
NA.22

ligand

pomalidomide

Assay

≥95%

Form

powder

Eignung der Reaktion

reactivity: amine reactive
reagent type: ligand-linker conjugate

Funktionelle Gruppe

carboxylic acid

Lagertemp.

2-8°C

SMILES String

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

Anwendung

Protein degrader builiding block Pomalidomide-PEG2-butyl CO2H 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 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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Piktogramme

Health hazard
GHS08

Signalwort

Danger

H-Sätze

H360D

Gefahreneinstufungen

Repr. 1B

Lagerklassenschlüssel

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Analysenzertifikate (COA)

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Die Dokumentenbibliothek aufrufen

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Molecular bioSystems, 7(2), 359-364 (2010-10-06)
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Angewandte Chemie (International ed. in English), 55(6), 1966-1973 (2016-01-13)
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Philipp M Cromm et al.
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Artikel

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.

Unser Team von Wissenschaftlern verfügt über Erfahrung in allen Forschungsbereichen einschließlich Life Science, Materialwissenschaften, chemischer Synthese, Chromatographie, Analytik und vielen mehr..

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