POMALIDOMIDE-DIFLUOROPEG1-C4-PIPERAZINE HYDROCHLORIDE (C005B-237217)

Application

Protein degrader building block Pomalidomide-difluoroPEG₁-C₄-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, a fluorinated linker with both hydrophobic and hydrophilic moieties, 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.

Targeted Protein Degradation

Other Notes

Impact of linker length on the activity of PROTACs

Targeted Protein Degradation: from Chemical Biology to Drug Discovery

Small-Molecule PROTACS: New Approaches to Protein Degradation

Targeted Protein Degradation by Small Molecules

Molecular Weight: 565.57 (free base basis). Empirical Formula: C₂₆H₃₃F₂N₅O₇ · xHCl. Quality Level: 100. Assay: ≥. 95%. form: powder. storage temp.: 2-8°C. SMILES string: O: C(C(CC1)N(C2: O)C(C3: C2C: CC: C3NC(COCC(F)(F)COCCCCN4CCNCC4): O): O)NC1: O.Cl. Pictograms: GHS08. Signal Word: Danger. Hazard Statements: H360D. Precautionary Statements: P201 - P202 - P280 - P308 + P313 - P405 - P501. Hazard Classifications: Repr. 1B. Storage Class Code: 6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.

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