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901829

Sigma-Aldrich

Pomalidomide-PEG6-CO2H

别名:

1-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-3,6,9,12,15,18-hexaoxahenicosan-21-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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About This Item

经验公式（希尔记法）:
C28H39N3O12
CAS号:
2225148-49-0
分子量:
609.62
MDL號碼:
MFCD32173791
分類程式碼代碼:
51171641
NACRES:
NA.22

ligand

pomalidomide

化驗

≥95%

形狀

liquid

反應適用性

reactivity: amine reactive
reagent type: ligand-linker conjugate

官能基

carboxylic acid

儲存溫度

2-8°C

SMILES 字串

O=C(NC1=O)CCC1N(C2=O)C(C3=C2C=CC=C3NCCOCCOCCOCCOCCOCCOCCC(O)=O)=O

InChI

1S/C28H39N3O12/c32-23-5-4-22(26(35)30-23)31-27(36)20-2-1-3-21(25(20)28(31)37)29-7-9-39-11-13-41-15-17-43-19-18-42-16-14-40-12-10-38-8-6-24(33)34/h1-3,22,29H,4-19H2,(H,33,34)(H,30,32,35)

InChI 密鑰

NBDBXIANAMQQQU-UHFFFAOYSA-N

相关类别

應用

Protein degrader builiding block Pomalidomide-PEG6-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)

其他說明

TTechnology 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 Degradations

Targeted Protein Degradation: from Chemical Biology to Drug Discovery

Impact of linker length on the activity of PROTACs

法律資訊

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

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产品编号
说明
价格

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Pomalidomide-PEG4-CO2H

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

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

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

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Pomalidomide-PEG2-azide

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Pomalidomide-PEG1-azide

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

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(S,R,S)-AHPC-PEG3-azide, ≥95%

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Pomalidomide-PEG2-butyl iodide, ≥95%

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

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Pomalidomide-PEG3-叠氮化物

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

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

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儲存類別代碼

10 - Combustible liquids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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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
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

商品

Partial PROTACs for Targeted Protein Degradation

Partial PROTACs are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

Degrader Building Blocks for Targeted Protein Degradation

Partial PROTACs are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

Partial PROTACs for Targeted Protein Degradation

Partial PROTACs are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

Degrader Building Blocks for Targeted Protein Degradation

Partial PROTACs are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

Global Trade Item Number

货号GTIN
901829-50MG4061835330683

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