Empirical Formula (Hill Notation): | C31H46N4O11 · xHCl |
Molecular Weight: | 650.72 (free base basis) |
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.
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,
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
assay | 95% |
form | powder or crystals |
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, O=C(C(CC1)N(C2=O)C(C3=C2C=CC=C3NC(COCCOCCOCCOCCOCCOCCCCCCN)=O)=O)NC1=O.Cl |
WGK Germany | WGK 3 |
Flash Point F | Not applicable |
Flash Point C | Not applicable |