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901824

Pomalidomide-PEG4-CO2H

Synonyme(s) :

1-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-3,6,9,12-tetraoxapentadecan-15-oic acid, Crosslinker–E3 Ligase ligand conjugate, Protein degrader building block for PROTAC® research, Template for synthesis of targeted protein degrader

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A propos de cet article

Formule empirique (notation de Hill) :
C24H31N3O10
Numéro CAS:
2138440-81-8
Poids moléculaire :
521.52
MDL number:
MFCD32173789
UNSPSC Code:
51171641
NACRES:
NA.22
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ligand

pomalidomide

Quality Level

200

form

solid

reaction suitability

reactivity: amine reactive, reagent type: ligand-linker conjugate

functional group

carboxylic acid

storage temp.

2-8°C

SMILES string

O=C(C(CC1)N(C2=O)C(C3=C2C=CC=C3NCCOCCOCCOCCOCCC(O)=O)=O)NC1=O

InChI

1S/C24H31N3O10/c28-19-5-4-18(22(31)26-19)27-23(32)16-2-1-3-17(21(16)24(27)33)25-7-9-35-11-13-37-15-14-36-12-10-34-8-6-20(29)30/h1-3,18,25H,4-15H2,(H,29,30)(H,26,28,31)

InChI key

CAANPUBZFFRWQP-UHFFFAOYSA-N

Application

Protein degrader builiding block Pomalidomide-PEG4-CO2H 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 carboxylic acid for reactivity with an amine 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 carboxyl 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)

Other Notes

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

Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8

Legal Information

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

Classe de stockage

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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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.

John M Hatcher et al.
ACS medicinal chemistry letters, 9(6), 540-545 (2018-06-26)
Cortistatin A is a natural product isolated from the marine sponge Corticium simplex and was found to be a potent and selective inhibitor of CDK8. Many synthetic groups have reported total syntheses of Cortistatin A; however, these syntheses require between
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
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Numéro d'article de commerce international

RéférenceGTIN
901824-50MG04061835330645