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901500

Sigma-Aldrich

Pomalidomide-C3-CO2H

≥95%

别名:

4-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)butanoic 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）:
C17H17N3O6
CAS号:
2225940-47-4
分子量:
359.33
MDL编号:
MFCD32173777
UNSPSC代码:
12352101
NACRES:
NA.22

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

运输

wet ice

储存温度

2-8°C

SMILES字符串

O=C(C(CC1)N(C2=O)C(C3=C2C=CC=C3NCCCC(O)=O)=O)NC1=O

InChI

1S/C17H17N3O6/c21-12-7-6-11(15(24)19-12)20-16(25)9-3-1-4-10(14(9)17(20)26)18-8-2-5-13(22)23/h1,3-4,11,18H,2,5-8H2,(H,22,23)(H,19,21,24)

InChI key

DXQHHPDVZILLOC-UHFFFAOYSA-N

相关类别

应用

Protein degrader builiding block Pomalidomide-C3-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 an alkyl-chain 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.

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

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储存分类代码

11 - Combustible Solids

WGK

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闪点(°F)

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闪点(°C)

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000200392
0000162887
0000200392
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0000119712

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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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