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901824

Pomalidomide-PEG₄-CO₂H

Name: Pomalidomide-PEG<SUB>4</SUB>-CO<SUB>2</SUB>H
Brand: ALDRICH

别名:

1-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-3,6,9,12-tetraoxapentadecan-15-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）:

C₂₄H₃₁N₃O₁₀

CAS号:

2138440-81-8

分子量:

521.52

MDL编号:

MFCD32173789

UNSPSC代码:

51171641

NACRES:

NA.22

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Sigma-Aldrich

901504

Pomalidomide-PEG₃-CO₂H

Sigma-Aldrich

901828

Pomalidomide-PEG₅-CO₂H

Sigma-Aldrich

QBD10244

Amino-dPEG^®₄-acid

Sigma-Aldrich

901500

Pomalidomide-C₃-CO₂H

Sigma-Aldrich

901526

Pomalidomide-PEG₂-CO₂H

Sigma-Aldrich

905224

Pomalidomide-PEG₆-butyl amine hydrochloride

Sigma-Aldrich

901829

Pomalidomide-PEG₆-CO₂H

Sigma-Aldrich

901525

Pomalidomide-C₉-CO₂H

Sigma-Aldrich

922021

Droplet generator chip - Droplet size variation

Sigma-Aldrich

901527

Pomalidomide-PEG₁-CO₂H

ligand

pomalidomide

表单

solid

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=C3NCCOCCOCCOCCOCCC(O)=O)=O)NC1=O

InChI

1S/C24H31N3O10/c28-19-5-4-18(22(31)26-19)27-23(32)16-2-1-3-17(21(16)24(27)33)25-7-9-35-11-13-37-15-14-36-12-10-34-8-6-20(29)30/h1-3,18,25H,4-15H2,(H,29,30)(H,26,28,31)

InChI key

CAANPUBZFFRWQP-UHFFFAOYSA-N

应用

Protein degrader builiding block Pomalidomide-PEG₄-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

Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8

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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Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8.

John M Hatcher et al.

ACS medicinal chemistry letters, 9(6), 540-545 (2018-06-26)

Cortistatin A is a natural product isolated from the marine sponge Corticium simplex and was found to be a potent and selective inhibitor of CDK8. Many synthetic groups have reported total syntheses of Cortistatin A; however, these syntheses require between

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-PEG4-CO2H

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属性

ligand

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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说明

应用

其他说明

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储存分类代码

WGK

闪点(°F)

闪点(°C)

文件

分析证书(COA)

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