905224

Pomalidomide-PEG₆-butyl amine hydrochloride

≥95%

• Synonym(s): 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
• Empirical Formula (Hill Notation): C₃₁H₄₆N₄O₁₁ · xHCl
• Molecular Weight: 650.72 (free base basis)
• MDL number: MFCD32173813
• UNSPSC Code: 12352101
• NACRES: NA.22

Properties

• ligand: pomalidomide
• assay: ≥95%
• form: powder or crystals
• reaction suitability: reactivity: carboxyl reactive; reagent type: ligand-linker conjugate
• functional group: amine
• storage temp.: 2-8°C
• SMILES string: O=C(C(CC1)N(C2=O)C(C3=C2C=CC=C3NC(COCCOCCOCCOCCOCCOCCCCCCN)=O)=O)NC1=O.Cl
• InChI key: CAPZWAWDFXEZTQ-UHFFFAOYSA-N

Description

Application

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.[1][2][3][4]

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.

Other Notes

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

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable