921327

C5 Lenalidomide-PEG₆-Butyl NH₂ hydrochloride

≥95%

• Synonym(e): 24-Amino-N-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)-3,6,9,12,15,18-hexaoxatetracosanamide hydrochloride, Crosslinker–E3 Ligase ligand conjugate, Protein degrader building block for PROTAC^® research, Template for synthesis of targeted protein degrader
• Empirische Formel (Hill-System): C₃₁H₄₈N₄O₁₀ · xHCl
• Molekulargewicht: 636.73 (free base basis)
• NACRES: NA.22

Eigenschaften

• ligand: C5 Lenalidomide
• Qualitätsniveau: 100
• Assay: ≥95%
• Form: powder or crystals
• Eignung der Reaktion: reactivity: carboxyl reactive; reagent type: ligand-linker conjugate
• Funktionelle Gruppe: amine
• Lagertemp.: 2-8°C
• SMILES String: O=C1N(C2CCC(NC2=O)=O)CC3=CC(NC(COCCOCCOCCOCCOCCOCCCCCCN)=O)=CC=C31.Cl

Beschreibung

Anwendung

Protein degrader builiding block C5 Lenalidomide-PEG6-Butyl NH2 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 PEGylated linker, 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 terminal amine, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

Technology Spotlight:Degrader Building Blocks for Targeted Protein Degradation

Portal:Building PROTAC^® Degraders for Targeted Protein Degradation

Sonstige Hinweise

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable