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927678

Sigma-Aldrich

Pomalidomide-difluoroPEG1-C4-piperazine Hydrochloride

≥95%

Synonyme(s) :

2-(2,2-Difluoro-3-(4-(piperazin-1-yl)butoxy)propoxy)-N-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)acetamide hydrochloride

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About This Item

Formule empirique (notation de Hill):
C26H33F2N5O7 · xHCl
Poids moléculaire :
565.57 (free base basis)
Code UNSPSC :
12352101
Nomenclature NACRES :
NA.21

ligand

pomalidomide

Niveau de qualité

100

Pureté

≥95%

Forme

powder

Température de stockage

2-8°C

Chaîne SMILES 

O=C(C(CC1)N(C2=O)C(C3=C2C=CC=C3NC(COCC(F)(F)COCCCCN4CCNCC4)=O)=O)NC1=O.Cl

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

Autres remarques

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

Pictogrammes

Health hazard
GHS08

Mention d'avertissement

Danger

Mentions de danger

H360D

Classification des risques

Repr. 1B

Code de la classe de stockage

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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Certificats d'analyse (COA)

Lot/Batch Number
0000164241
0000180862

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Daniel P Bondeson et al.
Annual review of pharmacology and toxicology, 57, 107-123 (2016-10-13)
Protein homeostasis networks are highly regulated systems responsible for maintaining the health and productivity of cells. Whereas therapeutics have been developed to disrupt protein homeostasis, more recently identified techniques have been used to repurpose homeostatic networks to effect degradation of
Kedra Cyrus et al.
Molecular bioSystems, 7(2), 359-364 (2010-10-06)
Conventional genetic approaches have provided a powerful tool in the study of proteins. However, these techniques often preclude selective manipulation of temporal and spatial protein functions, which is crucial for the investigation of dynamic cellular processes. To overcome these limitations
Philipp M Cromm et al.
Cell chemical biology, 24(9), 1181-1190 (2017-06-27)
Traditional pharmaceutical drug discovery is almost exclusively focused on directly controlling protein activity to cure diseases. Modulators of protein activity, especially inhibitors, are developed and applied at high concentration to achieve maximal effects. Thereby, reduced bioavailability and off-target effects can
Momar Toure et al.
Angewandte Chemie (International ed. in English), 55(6), 1966-1973 (2016-01-13)
The current inhibitor-based approach to therapeutics has inherent limitations owing to its occupancy-based model: 1) there is a need to maintain high systemic exposure to ensure sufficient in vivo inhibition, 2) high in vivo concentrations bring potential for off-target side effects, and 3) there is

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