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Merck

913987

Sigma-Aldrich

Pomalidomide-C6-PEG1-C3-PEG1-butyl amine hydrochloride

≥95%

Synonim(y):

6-((5-((6-aminohexyl)oxy)pentyl)oxy)-N-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)hexanamide HCl, Crosslinker−E3 Ligase ligand conjugate, Pomalidomide conjugate, Pomalidomide-6-5-6-NH2, Protein degrader building block for PROTAC® research, Template for synthesis of targeted protein degrader

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About This Item

Wzór empiryczny (zapis Hilla):
C30H44N4O7 · xHCl
Masa cząsteczkowa:
572.69 (free base basis)
Kod UNSPSC:
12352101

ligand

pomalidomide

Próba

≥95%

Postać

powder

przydatność reakcji

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

grupa funkcyjna

amine

temp. przechowywania

2-8°C

ciąg SMILES

O=C(C(CC1)N(C2=O)C(C3=C2C=CC=C3NC(CCCCCOCCCCCOCCCCCCN)=O)=O)NC1=O.Cl

Zastosowanie

Protein degrader building block Pomalidomide-C6-PEG1-C3-PEG1-butyl amine hydrochloride 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 amine for reactivity with an acid on the target warhead. 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 terminal amine, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

Informacje prawne

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

Numer produktu
Opis
Cennik

Kod klasy składowania

11 - Combustible Solids

Klasa zagrożenia wodnego (WGK)

WGK 3

Temperatura zapłonu (°F)

Not applicable

Temperatura zapłonu (°C)

Not applicable


Certyfikaty analizy (CoA)

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Dokumenty związane z niedawno zakupionymi produktami zostały zamieszczone w Bibliotece dokumentów.

Odwiedź Bibliotekę dokumentów

Ashton C Lai et al.
Angewandte Chemie (International ed. in English), 55(2), 807-810 (2015-11-26)
Proteolysis Targeting Chimera (PROTAC) technology is a rapidly emerging alternative therapeutic strategy with the potential to address many of the challenges currently faced in modern drug development programs. PROTAC technology employs small molecules that recruit target proteins for ubiquitination and
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
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

Produkty

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

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