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Merck

905224

Sigma-Aldrich

Pomalidomide-PEG6-butyl amine hydrochloride

≥95%

Sinónimos:

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

Fórmula empírica (notación de Hill):
C31H46N4O11 · xHCl
Peso molecular:
650.72 (free base basis)
Código UNSPSC:
12352101

Análisis

≥95%

formulario

powder or crystals

idoneidad de la reacción

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

grupo funcional

amine

temp. de almacenamiento

2-8°C

cadena SMILES

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

Aplicación

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.

Información legal

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

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable


Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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Visite la Librería de documentos

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)

Artículos

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

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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