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Key Documents

905224

Sigma-Aldrich

Pomalidomide-PEG6-butyl amine hydrochloride

≥95%

Sinonimo/i:

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

Formula empirica (notazione di Hill):
C31H46N4O11 · xHCl
Peso molecolare:
650.72 (free base basis)
Codice UNSPSC:
12352101
NACRES:
NA.22

ligand

pomalidomide

Saggio

≥95%

Forma fisica

powder or crystals

Impiego in reazioni chimiche

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

Gruppo funzionale

amine

Temperatura di conservazione

2-8°C

Stringa SMILE

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

Applicazioni

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.

Note legali

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

Prodotti correlati

N° Catalogo
Descrizione
Determinazione del prezzo

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable


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Impact of linker length on the activity of PROTACs.
Cyrus K, et al.
Molecular Biosystems, 7(2), 359-364 (2011)
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)
Targeted protein degradation: from chemical biology to drug discovery.
Cromm, Philipp M and Crews, Craig M
Cell Chemical Biology, 24(9), 1181-1190 (2017)

Articoli

Partial PROTACs are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

Partial PROTACs are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

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