Accéder au contenu
MilliporeSigma
Toutes les photos(1)

Documents

911747

Sigma-Aldrich

C5 Lenalidomide-PEG3-NH2 hydrochloride

≥95%

Synonyme(s) :

2-(2-(2-(2-Aminoethoxy)ethoxy)ethoxy)-N-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)acetamide hydrochloride, C5 Lenalidomide conjugate, Crosslinker–E3 Ligase ligand conjugate, Protein degrader building block for PROTAC® research, Template for synthesis of targeted protein degrader

Se connecterpour consulter vos tarifs contractuels et ceux de votre entreprise/organisme
Toutes les photos(1)

About This Item

Formule empirique (notation de Hill):
C21H28N4O7 · xHCl
Poids moléculaire :
448.47 (free base basis)
Code UNSPSC :
12352101

ligand

C5 Lenalidomide

Pureté

≥95%

Forme

powder or crystals

Pertinence de la réaction

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

Groupe fonctionnel

amine

Température de stockage

2-8°C

Chaîne SMILES 

O=C1N(C2CCC(NC2=O)=O)CC3=CC(NC(COCCOCCOCCN)=O)=CC=C31.Cl

Application

Protein degrader builiding block C5 Lenalidomide-PEG3-NH2 hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand with alternative exit vector and a PEGylated crosslinker with pendant amine for reactivity with an acid on the target warhead. Because even slight alterations in ligands, warheads, 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 terminal amine, 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)

Autres remarques

Degrader Building Blocks for Targeted Protein Degradation.

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

Informations légales

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

Produit(s) apparenté(s)

Réf. du produit
Description
Tarif

901488

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

901493

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

901495

Pomalidomide-PEG3-NH2 hydrochloride, ≥95%

901511

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

901516

Pomalidomide-PEG1-NH2 hydrochloride, ≥95%

901513

Pomalidomide-PEG2-NH2 hydrochloride, ≥95%

901832

Pomalidomide-PEG6-NH2 hydrochloride, ≥98%

901831

Pomalidomide-PEG5-NH2 hydrochloride

901830

Pomalidomide-PEG4-NH2 hydrochloride, ≥95%

901860

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

901850

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

901848

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

905275

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

906123

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

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%

911720

C5 Lenalidomide-C9-NH2 hydrochloride, ≥95%

911712

C5 Lenalidomine-C6-NH2 hydrochloride, ≥95%

911755

C5 Lenalidomide-PEG5-NH2 hydrochloride

911704

C5 Lenalidomine-C3-NH2 hydrochloride, ≥95%

911739

C5 Lenalidomide-PEG1-NH2 hydrochloride, ≥95%

911747

C5 Lenalidomide-PEG3-NH2 hydrochloride, ≥95%

911771

Lenalidomide-Photoswitch1-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%

917052

(S,R,S)-AHPC-C3-NH2 hydrochloride, ≥95%

917818

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

917559

(S,R,S)-AHPC-C6-NH2 hydrochloride, ≥95%

919357

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

918350

C5 Lenalidomide-alkyne-piperidine hydrochloride, ≥95%

919454

CCW16-PEG3-BocNH, ≥95%

919969

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

919896

C5 Lenalidomide-dipiperazine-NH2 hydrochloride

920746

Pomalidomide-benzyl-piperazine hydrochloride

920754

C5 Lenalidomide-benzyl-piperazine hydrochloride

920789

Pomalidomide-pyridine-PEG1-piperazine hydrochloride

920797

C5 Lenalidomide-pyridine-PEG1-piperazine hydrochloride, ≥95%

920800

C5 Lenalidomide-methylamino-PEG1-NH2 hydrochloride, ≥95%

921300

C5 Lenalidomide-pyrimidine-piperazine-PEG1-NH2 hydrochloride, ≥95%

921327

C5 Lenalidomide-PEG6-Butyl NH2 hydrochloride, ≥95%

924202

5-Amino-Thalidomide, ≥95%

Pictogrammes

Health hazard
GHS08

Mention d'avertissement

Warning

Mentions de danger

H361d,H373

Conseils de prudence

P201 - P308 + P313

Classification des risques

Repr. 2 - STOT RE 2

Organes cibles

Blood

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 1

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".

Déjà en possession de ce produit ?

Retrouvez la documentation relative aux produits que vous avez récemment achetés dans la Bibliothèque de documents.

Consulter la Bibliothèque de documents

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
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

Articles

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.

Notre équipe de scientifiques dispose d'une expérience dans tous les secteurs de la recherche, notamment en sciences de la vie, science des matériaux, synthèse chimique, chromatographie, analyse et dans de nombreux autres domaines..

Contacter notre Service technique