910449

Pomalidomide-PEG₂-butyl CO₂H

≥95%

• Sinônimo(s): 7-(2-(2-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-2-oxoethoxy)ethoxy)heptanoic acid, Crosslinker−E3 ligase ligand conjugate, Pomalidomide conjugate, Pomalidomide-2-2-6-acid, Protein degrader building block for PROTAC^® research, Template for synthesis of targeted protein degrader
• Fórmula empírica (Notação de Hill): C₂₄H₂₉N₃O₉
• Peso molecular: 503.50
• Número MDL: MFCD32669897
• Código UNSPSC: 12352101
• NACRES: NA.22

Propriedades

• ligand: pomalidomide
• Ensaio: ≥95%
• Formulário: powder
• adequação da reação: reactivity: amine reactive; reagent type: ligand-linker conjugate
• grupo funcional: carboxylic acid
• temperatura de armazenamento: 2-8°C
• cadeia de caracteres SMILES: O=C(C(CC1)N(C2=O)C(C3=C2C=CC=C3NC(COCCOCCCCCCC(O)=O)=O)=O)NC1=O
• InChI: 1S/C24H29N3O9/c28-18-10-9-17(22(32)26-18)27-23(33)15-6-5-7-16(21(15)24(27)34)25-19(29)14-36-13-12-35-11-4-2-1-3-8-20(30)31/h5-7,17H,1-4,8-14H2,(H,25,29)(H,30,31)(H,26,28,32)
• chave InChI: PTXYFBNBOJXGJO-UHFFFAOYSA-N

Descrição

Aplicação

Protein degrader builiding block Pomalidomide-PEG₂-butyl CO₂H 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 carboxylic acid for reactivity with an amine 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 carboxyl group, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

Outras notas

Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation

Portal: Building PROTAC^® Degraders for Targeted Protein Degradation

Targeted Protein Degradation by Small Molecules

Small-Molecule PROTACS: New Approaches to Protein Degradation

Targeted Protein Degradation: from Chemical Biology to Drug Discovery

Impact of linker length on the activity of PROTACs

Informações legais

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

Informações de segurança

• Pictogramas: GHS08
• Palavra indicadora: Danger
• Frases de perigo: H360D
• Declarações de precaução: P201 - P202 - P280 - P308 + P313 - P405 - P501
• Classificações de perigo: Repr. 1B
• Código de classe de armazenamento: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable