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Merck

905224

Sigma-Aldrich

Pomalidomide-PEG6-butyl amine hydrochloride

≥95%

Synonim(y):

24-Amino-N-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin, Crosslinker–E3 Ligase ligand conjugate, Pomalidomide-2-2-2-2-2-2-6-NH2 HCl salt, 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):
C31H46N4O11 · xHCl
Masa cząsteczkowa:
650.72 (free base basis)
Kod UNSPSC:
12352101
NACRES:
NA.22

ligand

pomalidomide

Próba

≥95%

Postać

powder or crystals

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(COCCOCCOCCOCCOCCOCCCCCCN)=O)=O)NC1=O.Cl

Zastosowanie

Partial PROTAC Pomalidomide-PEG6-butyl amine (HCl salt) 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 a carboxyl group 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 Partial PROTACs with a pendant amine, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.
Protein degrader builiding block Pomalidomide-PEG6-Butyl Amine (HCl salt) 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 a carboxyl group 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 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)

Poszukaj Certyfikaty analizy (CoA), wpisując numer partii/serii produktów. Numery serii i partii można znaleźć na etykiecie produktu po słowach „seria” lub „partia”.

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

Odwiedź Bibliotekę dokumentów

Targeted protein degradation by small molecules.
Bondeson DP and Crews CM
Annual Review of Pharmacology and Toxicology, 57(9), 107-123 (2017)
Targeted protein degradation by PROTACs.
Neklesa TK, et al.
Pharmacology & Therapeutics, 174, 138-144 (2017)
Impact of linker length on the activity of PROTACs.
Cyrus K, et al.
Molecular Biosystems, 7(2), 359-364 (2011)
Targeted protein degradation: from chemical biology to drug discovery.
Cromm, Philipp M and Crews, Craig M
Cell Chemical Biology, 24(9), 1181-1190 (2017)

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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