920797

C5 Lenalidomide-pyridine-PEG₁-piperazine hydrochloride

≥95%

• Synonyme(s) : N-(2-(2,6-Dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)-2-(6-(3-(piperazin-1-yl)propoxy)pyridin-3-yl)acetamide hydrochloride, Crosslinker−E3 Ligase ligand conjugate, Protein degrader building block for PROTAC^® research, Template for synthesis of targeted protein degrader
• Formule empirique (notation de Hill): C₂₇H₃₂N₆O₅ · xHCl
• Poids moléculaire : 520.58 (free base basis)
• Code UNSPSC : 12352101
• Nomenclature NACRES : NA.22

Propriétés

• ligand: C5 Lenalidomide
• Niveau de qualité: 100
• Pureté: ≥95%
• Forme: powder or crystals
• Pertinence de la réaction: reactivity: carboxyl reactive; reagent type: ligand-linker conjugate
• Groupe fonctionnel: amine
• Température de stockage: 2-8°C
• Chaîne SMILES: O=C1N(C2CCC(NC2=O)=O)CC3=CC(NC(CC4=CC=C(OCCCN5CCNCC5)N=C4)=O)=CC=C31.Cl

Description

Application

Protein degrader building block C5 Lenalidomide-pyridine-PEG₁-piperazine hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand with alternative exit vector, a linker with added rigidity, and a pendant amine for reactivity with a carboxylic acid 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.

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable