901835
Pomalidomide-PEG6-Alkyne
동의어(들):
N-(2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)-4,7,10,13,16,19-hexaoxadocos-21-ynamide, Crosslinker–E3 Ligase ligand conjugate, Protein degrader building block for PROTAC® research, Template for synthesis of targeted protein degrader
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제품정보 (DICE 배송 시 비용 별도)
실험식(Hill 표기법):
C29H37N3O11
Molecular Weight:
603.62
UNSPSC Code:
51171641
NACRES:
NA.22
ligand
pomalidomide
form
powder or chunks
reaction suitability
reaction type: click chemistry, reagent type: ligand-linker conjugate
mp
279-284 °C
functional group
alkyne
storage temp.
2-8°C
SMILES string
O=C(C(CC1)N(C2=O)C(C3=C2C=CC=C3NC(CCOCCOCCOCCOCCOCCOCC#C)=O)=O)NC1=O
Application
Protein degrader builiding block Pomalidomide-PEG6-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)
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
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
Legal Information
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
저장 등급
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
문서
Protein Degrader Building Blocks are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.
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
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
국제 무역 품목 번호
| SKU | GTIN |
|---|---|
| 901835-50MG | 04061835330805 |