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911720

Sigma-Aldrich

C5 Lenalidomide-C9-NH2 hydrochloride

≥95%

Sinonimo/i:

10-amino-N-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)decanamide hydrochloride, C5 Lenalidomide conjugate, 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):
C23H32N4O4 · xHCl
Peso molecolare:
428.52 (free base basis)
Codice UNSPSC:
12352101
NACRES:
NA.22

ligand

C5 Lenalidomide

Livello qualitativo

Saggio

≥95%

Forma fisica

powder

Impiego in reazioni chimiche

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

Gruppo funzionale

amine

Temperatura di conservazione

2-8°C

Stringa SMILE

O=C1N(C2CCC(NC2=O)=O)CC3=CC(NC(CCCCCCCCCN)=O)=CC=C31.Cl

Applicazioni

Protein degrader building block C5 Lenalidomide-C9-NH2 hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand with alternative exit vector and a PEGylated crosslinker with pendant amine for reactivity with an acid on the target warhead. Because even slight alterations in ligands, warheads, 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 terminal amine, 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

Warning

Indicazioni di pericolo

Classi di pericolo

Repr. 2 - STOT RE 2

Organi bersaglio

Blood

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 1

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable


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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
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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