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910449

Sigma-Aldrich

Pomalidomide-PEG2-butyl CO2H

≥95%

Sinonimo/i:

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

Formula empirica (notazione di Hill):
C24H29N3O9
Peso molecolare:
503.50
Codice UNSPSC:
12352101
NACRES:
NA.22

ligand

pomalidomide

Saggio

≥95%

Forma fisica

powder

Impiego in reazioni chimiche

reactivity: amine reactive
reagent type: ligand-linker conjugate

Gruppo funzionale

carboxylic acid

Temperatura di conservazione

2-8°C

Stringa SMILE

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

Applicazioni

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.

Note legali

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

Prodotti correlati

N° Catalogo
Descrizione
Determinazione del prezzo

Pittogrammi

Health hazard

Avvertenze

Danger

Indicazioni di pericolo

Classi di pericolo

Repr. 1B

Codice della classe di stoccaggio

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

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable


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Kedra Cyrus et al.
Molecular bioSystems, 7(2), 359-364 (2010-10-06)
Conventional genetic approaches have provided a powerful tool in the study of proteins. However, these techniques often preclude selective manipulation of temporal and spatial protein functions, which is crucial for the investigation of dynamic cellular processes. To overcome these limitations
Momar Toure et al.
Angewandte Chemie (International ed. in English), 55(6), 1966-1973 (2016-01-13)
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
Philipp M Cromm et al.
Cell chemical biology, 24(9), 1181-1190 (2017-06-27)
Traditional pharmaceutical drug discovery is almost exclusively focused on directly controlling protein activity to cure diseases. Modulators of protein activity, especially inhibitors, are developed and applied at high concentration to achieve maximal effects. Thereby, reduced bioavailability and off-target effects can

Articoli

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

Il team dei nostri ricercatori vanta grande esperienza in tutte le aree della ricerca quali Life Science, scienza dei materiali, sintesi chimica, cromatografia, discipline analitiche, ecc..

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