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901526

Pomalidomide-PEG₂-CO₂H

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

95%

别名:

3-(2-(2-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethoxy)ethoxy)propanoic acid, CrosslinkerE3 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）:

C₂₀H₂₃N₃O₈

CAS号:

2140807-17-4

分子量:

433.41

MDL编号:

MFCD32173785

UNSPSC代码:

51171641

NACRES:

NA.22

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Sigma-Aldrich

901504

Pomalidomide-PEG₃-CO₂H

Sigma-Aldrich

900913

四嗪-五聚乙二醇-活性脂

Sigma-Aldrich

901525

Pomalidomide-C₉-CO₂H

Sigma-Aldrich

901824

Pomalidomide-PEG₄-CO₂H

Sigma-Aldrich

901496

Pomalidomide-C₆-CO₂H

Sigma-Aldrich

901495

Pomalidomide-PEG₃-NH₂ hydrochloride

Sigma-Aldrich

909408

Pomalidomide-PEG₆-azide

Sigma-Aldrich

901516

Pomalidomide-PEG₁-NH₂hydrochloride

Sigma-Aldrich

790451

TCO-amine HCl salt

Sigma-Aldrich

901513

Pomalidomide-PEG₂-NH₂ hydrochloride

ligand

pomalidomide

质量水平

100

方案

95%

表单

powder or crystals

反应适用性

reactivity: amine reactive
reagent type: ligand-linker conjugate

官能团

carboxylic acid

储存温度

2-8°C

SMILES字符串

O=C(C(CC1)N(C2=O)C(C3=C2C=CC=C3NCCOCCOCCC(O)=O)=O)NC1=O

InChI

1S/C20H23N3O8/c24-15-5-4-14(18(27)22-15)23-19(28)12-2-1-3-13(17(12)20(23)29)21-7-9-31-11-10-30-8-6-16(25)26/h1-3,14,21H,4-11H2,(H,25,26)(H,22,24,27)

InChI key

NKISJPXMSOQWER-UHFFFAOYSA-N

应用

Protein degrader builiding block Pomalidomide-PEG₂-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)

其他说明

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

法律信息

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

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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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

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.

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Pomalidomide-PEG2-CO2H

95%

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ligand

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方案

表单

反应适用性

官能团

储存温度

SMILES字符串

InChI

InChI key

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其他说明

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储存分类代码

WGK

闪点(°F)

闪点(°C)

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