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文件

911003

Pomalidomide-PEG₂-butyl amine hydrochloride

Name: Pomalidomide-PEG<SUB>2</SUB>-butyl amine hydrochloride
Brand: ALDRICH

≥95%

别名:

2-(2-((6-Aminohexyl)oxy)ethoxy)-N-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)acetamide hydrochloride, Crosslinker−E3 Ligase ligand conjugate, Pomalidomide conjugate, Pomalidomide-2-2-6-NH₂ HCl salt, 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）:

C₂₃H₃₀N₄O₇

分子量:

474.51

分類程式碼代碼:

12352101

ligand

pomalidomide

化驗

≥95%

形狀

solid

反應適用性

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

官能基

amine

儲存溫度

2-8°C

SMILES 字串

O=C(C(CC1)N(C2=O)C(C3=C2C=CC=C3NC(COCCOCCCCCCN)=O)=O)NC1=O.Cl

應用

Protein degrader builiding block Pomalidomide-PEG₂-butyl amine hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand, a linker with both hydrophobic and hydrophilic moieties, and a pendant amine acid for reactivity with a carboxylic acid 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 amine, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

其他說明

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

法律資訊

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

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

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Impact of linker length on the activity of PROTACs.

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

Small-Molecule PROTACS: New Approaches to Protein Degradation.

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

Targeted Protein Degradation: from Chemical Biology to Drug Discovery.

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

商品

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.

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.

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.

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.

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Pomalidomide-PEG2-butyl amine hydrochloride

≥95%

About This Item

属性

ligand

化驗

形狀

反應適用性

官能基

儲存溫度

SMILES 字串

说明

應用

其他說明

法律資訊

相关产品

相關產品

安全信息

儲存類別代碼

水污染物質分類（WGK）

閃點（°F）

閃點（°C）

文件

分析证书(COA)

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Pomalidomide-PEG₂-butyl amine hydrochloride