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901529

Pomalidomide-PEG₂-Alkyne

Name: Pomalidomide-PEG<SUB>2</SUB>-Alkyne
Brand: ALDRICH

≥95%

别名:

N-(2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)-3-(2-(prop-2-yn-1-yloxy)ethoxy)propanamide, 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）:

C₂₁H₂₁N₃O₇

分子量:

427.41

分類程式碼代碼:

51171641

NACRES:

NA.22

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Slide 1 of 10

1 of 10

Sigma-Aldrich

901531

Pomalidomide-PEG₃-Alkyne

Sigma-Aldrich

904678

Pomalidomide-PEG3-叠氮化物

Sigma-Aldrich

909394

Pomalidomide-PEG₅-azide

Sigma-Aldrich

689807

甲氧基聚乙二醇叠氮化物

Sigma-Aldrich

903833

Pomalidomide-PEG2-azide

Sigma-Aldrich

920738

Pomalidomide-C9-NH₂ hydrochloride

Sigma-Aldrich

903434

Pomalidomide-PEG₆-butyl azide

Sigma-Aldrich

930563

Pomalidomide-PEG₂-C₂-azide

Sigma-Aldrich

689475

甲氧基聚乙二醇叠氮化物

Sigma-Aldrich

727423

2-[2-(2-氨基乙氧基)乙氧基]乙醇溶液

ligand

pomalidomide

品質等級

100

化驗

≥95%

形狀

powder or crystals

反應適用性

reaction type: click chemistry
reagent type: ligand-linker conjugate

官能基

alkyne

儲存溫度

2-8°C

SMILES 字串

O=C(C(CC1)N(C2=O)C(C3=C2C=CC=C3NC(CCOCCOCC#C)=O)=O)NC1=O

應用

Protein degrader builiding block Pomalidomide-PEG₂-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)

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

从最新的版本中选择一种：

分析证书(COA)

Lot/Batch Number

MKCG6063

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Slide 1 of 5

1 of 5

Sigma-Aldrich

901516

Pomalidomide-PEG₁-NH₂hydrochloride

Sigma-Aldrich

904724

Pomalidomide-PEG₂-butyl iodide

Sigma-Aldrich

901495

Pomalidomide-PEG₃-NH₂ hydrochloride

Sigma-Aldrich

P0018

泊马度胺

Sigma-Aldrich

901558

来那度胺

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

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

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

Targeted Protein Degradation by Small Molecules.

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.

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Key Documents

Pomalidomide-PEG2-Alkyne

≥95%

About This Item

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属性

ligand

品質等級

化驗

形狀

反應適用性

官能基

儲存溫度

SMILES 字串

相关类别

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-Alkyne