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901531

Sigma-Aldrich

Pomalidomide-PEG3-Alkyne

≥95%

Sinonimo/i:

N-(2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)-3-(2-(2-(prop-2-yn-1-yloxy)ethoxy)ethoxy)propanamide, Crosslinker−E3 Ligase ligand conjugate, Protein degrader building block for PROTAC® research, Template for synthesis of targeted protein degrader

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About This Item

Formula empirica (notazione di Hill):
C23H25N3O8
Peso molecolare:
471.46
Codice UNSPSC:
51171641
NACRES:
NA.22

ligand

pomalidomide

Livello qualitativo

100

Saggio

≥95%

Forma fisica

powder or crystals

Impiego in reazioni chimiche

reaction type: click chemistry
reagent type: ligand-linker conjugate

Gruppo funzionale

alkyne

Temperatura di conservazione

2-8°C

Stringa SMILE

O=C(C(CC1)N(C2=O)C(C3=C2C=CC=C3NC(CCOCCOCCOCC#C)=O)=O)NC1=O

Categorie correlate

Applicazioni

Protein degrader builiding block Pomalidomide-PEG3-Alkyne enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand and a PEGylated crosslinker with pendant alkyne for click chemistry with an azide 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 alkyne group, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

Automate your CRBN-PEG based PROTACs with Synple Automated Synthesis Platform (SYNPLE-SC002)

Altre note

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 ProteinDegradation

Targeted Protein Degradation: from ChemicalBiology to Drug Discovery

Impact of linker length on the activity of PROTACs

Note legali

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

Prodotti correlati

N° Catalogo
Descrizione
Determinazione del prezzo

P0018

Pomalidomide, ≥98% (HPLC)

901488

(S,R,S)-AHPC-PEG2-NH2 hydrochloride, ≥95%

901493

(S,R,S)-AHPC-PEG1-NH2 hydrochloride, ≥95%

901494

N-Methylated pomalidomide, ≥98%

901495

Pomalidomide-PEG3-NH2 hydrochloride, ≥95%

901496

Pomalidomide-C6-CO2H, ≥98%

901500

Pomalidomide-C3-CO2H, ≥95%

901503

(S,R,S)-AHPC-PEG1-Alkyne, ≥95%

901511

(S,R,S)-AHPC-PEG3-NH2 hydrochloride, ≥95%

901504

Pomalidomide-PEG3-CO2H, ≥95%

901517

(S,R,S)-AHPC-PEG2-Alkyne, ≥95%

901516

Pomalidomide-PEG1-NH2 hydrochloride, ≥95%

901513

Pomalidomide-PEG2-NH2 hydrochloride, ≥95%

901523

Pomalidomide-PEG1-Alkyne, ≥98%

901533

(S,R,S)-AHPC-PEG3-Alkyne, ≥95%

901534

(S,R,S)-AHPC-C6-CO2H hydrochloride

901531

Pomalidomide-PEG3-Alkyne, ≥95%

901529

Pomalidomide-PEG2-Alkyne, ≥95%

901527

Pomalidomide-PEG1-CO2H, ≥95%

901526

Pomalidomide-PEG2-CO2H, 95%

901525

Pomalidomide-C9-CO2H, ≥95%

901558

Lenalidomide, ≥95%

901835

Pomalidomide-PEG6-Alkyne

901834

Pomalidomide-PEG5-Alkyne, ≥95%

901833

Pomalidomide-PEG4-Alkyne

901832

Pomalidomide-PEG6-NH2 hydrochloride, ≥98%

901831

Pomalidomide-PEG5-NH2 hydrochloride

901830

Pomalidomide-PEG4-NH2 hydrochloride, ≥95%

901829

Pomalidomide-PEG6-CO2H

901828

Pomalidomide-PEG5-CO2H, ≥95%

901824

Pomalidomide-PEG4-CO2H

901860

(S,R,S)-AHPC-PEG6-NH2 hydrochloride, ≥95%

901855

(S,R,S)-AHPC-PEG5-Alkyne

901851

(S,R,S)-AHPC-PEG4-Alkyne

901850

(S,R,S)-AHPC-PEG5-NH2 hydrochloride

901848

(S,R,S)-AHPC-PEG4-NH2 hydrochloride, ≥95%

901873

(S,R,S)-AHPC-PEG6-Alkyne

903434

Pomalidomide-PEG6-butyl azide, ≥95%

903442

Pomalidomide-PEG6-butyl iodide, ≥95%

903833

Pomalidomide-PEG2-azide

903825

Pomalidomide-PEG1-azide

903957

(S,R,S)-AHPC-PEG1-azide

904651

(S,R,S)-AHPC-PEG3-azide, ≥95%

904724

Pomalidomide-PEG2-butyl iodide, ≥95%

904708

Pomalidomide-C6-PEG3-butyl iodide, ≥95%

904678

Pomalidomide-PEG3-azide

904686

Pomalidomide-C6-PEG3-butyl azide, ≥95%

904813

(S,R,S)-AHPC-PEG2-azide

904821

(S,R,S)-AHPC-C6-PEG3-butyl azide, ≥95%

904880

Pomalidomide-C6-PEG1-C3-PEG1-butyl azide, ≥95%

904872

Pomalidomide-PEG2-butyl azide, ≥95%

904864

(S,R,S)-AHPC-PEG6-butyl azide, ≥95%

905178

(S,R,S)-AHPC-C6-PEG1-C3-PEG1-butyl azide, ≥95%

905275

(S,R,S)-AHPC-PEG6-butyl amine hydrochloride, ≥95%

905216

(S,R,S)-AHPC-PEG2-butyl azide, ≥95%

905232

(S,R,S)-AHPC-C6-PEG3-butyl amine hydrochloride, ≥95%

905224

Pomalidomide-PEG6-butyl amine hydrochloride, ≥95%

905208

Pomalidomide-C6-PEG3-butyl amine hydrochloride, ≥98%

905399

(S,R,S)-AHPC-PEG2-butyl chloride

905380

(S,R,S)-AHPC-C6-PEG3-butyl chloride, ≥95%

905402

(S,R,S)-AHPC-C6-PEG1-C3-PEG1-butyl chloride, 95%

906050

Pomalidomide-C6-PEG1-C3-PEG1-butyl iodide, ≥95%

906123

(S,R,S)-AHPC-PEG2-butyl amine hydrochloride

907677

(S,R,S)-AHPC-PEG6-butyl chloride

909378

(S,R,S)-AHPC-PEG6-Azide, ≥95%

909386

Pomalidomide-PEG4-Azide, ≥95%

909394

Pomalidomide-PEG5-azide, ≥95%

909408

Pomalidomide-PEG6-azide, ≥95%

909262

(S,R,S)-AHPC-PEG4-Azide, ≥95%

910449

Pomalidomide-PEG2-butyl CO2H, ≥95%

910600

(S,R,S)-AHPC-PEG2-butyl CO2H, ≥95%

910619

Pomalidomide-PEG6-butyl alkyne, ≥95%

910597

(S,R,S)-AHPC-PEG6-butyl alkyne, ≥95%

910554

(S,R,S)-AHPC-PEG6-butyl CO2H, ≥95%

910546

(S,R,S)-AHPC-C6-PEG3-butyl alkyne, ≥95%

910538

(S,R,S)-AHPC-PEG2-butyl alkyne, ≥95%

910511

Pomalidomide-C6-PEG3-butyl alkyne, ≥95.0%

910503

Pomalidomide-PEG2-butyl alkyne, ≥95%

910481

Pomalidomide-PEG6-butyl CO2H, ≥95%

911003

Pomalidomide-PEG2-butyl amine hydrochloride, ≥95%

911801

AHPC-C6-PEG1-C3-PEG1-butyl amine hydrochloride, ≥90%

911690

C5 Lenalidomide, ≥95%

911666

Pomalidomide-C6-NH2 hydrochloride, ≥95%

911658

Pomalidomide-C3-NH2 hydrochloride, ≥95%

911763

C5 Lenalidomide-PEG1-piperazine hydrochloride, ≥95%

913987

Pomalidomide-C6-PEG1-C3-PEG1-butyl amine hydrochloride, ≥95%

915572

Pomalidomide-dipiperazine-NH2 hydrochloride, ≥95%

916536

Pomalidomide-piperazine-pyridine-alkyne-NH2 hydrochloride

917729

C5 Lenalidomide-piperazine-pyridine-alkyne-NH2 hydrochloride, ≥95%

917303

C5 Lenalidomide-C6-PEG1-C3-PEG1-Butyl NH2 hydrochloride, ≥95%

917818

(S,R,S)-AHPC-C9-NH2 hydrochloride, ≥95%

919454

CCW16-PEG3-BocNH, ≥95%

918687

(S,R,S)-AHPC-alkyne-piperidine hydrochloride

919969

C5 Lenalidomide-PEG2-Butyl NH2 hydrochloride, ≥95%

919896

C5 Lenalidomide-dipiperazine-NH2 hydrochloride

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Certificati d'analisi (COA)

Cerca il Certificati d'analisi (COA) digitando il numero di lotto/batch corrispondente. I numeri di lotto o di batch sono stampati sull'etichetta dei prodotti dopo la parola ‘Lotto’ o ‘Batch’.

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Pomalidomide ≥98% (HPLC)

Sigma-Aldrich

P0018

Pomalidomide

Pomalidomide-C3-CO2H ≥95%

Sigma-Aldrich

901500

Pomalidomide-C3-CO2H

(S,R,S)-AHPC-PEG1-azide

Sigma-Aldrich

903957

(S,R,S)-AHPC-PEG1-azide

Lenalidomide ≥95%

Sigma-Aldrich

901558

Lenalidomide

Pomalidomide-PEG1-azide

Sigma-Aldrich

903825

Pomalidomide-PEG1-azide

N-Methylated pomalidomide ≥98%

Sigma-Aldrich

901494

N-Methylated pomalidomide

(±)-Thalidomide ≥98%, powder

Sigma-Aldrich

T144

(±)-Thalidomide

4-(Acetylamino)phenyl]imidodisulfuryl difluoride ≥98%

Sigma-Aldrich

901243

4-(Acetylamino)phenyl]imidodisulfuryl difluoride

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
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
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
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

Articoli

Degrader Building Blocks for Targeted Protein Degradation

Protein Degrader Building Blocks are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

Il team dei nostri ricercatori vanta grande esperienza in tutte le aree della ricerca quali Life Science, scienza dei materiali, sintesi chimica, cromatografia, discipline analitiche, ecc..

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