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909386

Pomalidomide-PEG₄-Azide

Name: Pomalidomide-PEG<SUB>4</SUB>-Azide
Brand: ALDRICH

≥95%

别名:

14-Azido-N-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)-3,6,9,12-tetraoxatetradecanamide, Crosslinker-E3 ligase ligand conjugate, Pomalidomide 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）:

C₂₃H₂₈N₆O₉

分子量:

532.50

MDL號碼:

MFCD32197465

分類程式碼代碼:

51171641

NACRES:

NA.22

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Sigma-Aldrich

SML3900

955, CDK9 PROTAC trifluoroacetate

Sigma-Aldrich

920746

Pomalidomide-benzyl-piperazine hydrochloride

Sigma-Aldrich

901495

Pomalidomide-PEG₃-NH₂ hydrochloride

Sigma-Aldrich

904678

Pomalidomide-PEG3-叠氮化物

Sigma-Aldrich

917435

BocA1V1PF2-OPEG₁-NH₂hydrochloride

Sigma-Aldrich

E4876

17α-乙炔基雌二醇

Sigma-Aldrich

P0018

泊马度胺

Sigma-Aldrich

L6545

来曲唑

Sigma-Aldrich

903825

Pomalidomide-PEG1-azide

Sigma-Aldrich

SML1896

VH298

ligand

pomalidomide

化驗

≥95%

形狀

powder or solid

反應適用性

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

官能基

azide

儲存溫度

2-8°C

SMILES 字串

O=C(C(CC1)N(C2=O)C(C3=C2C=CC=C3NC(COCCOCCOCCOCCN=[N+]=[N-])=O)=O)NC1=O

InChI

1S/C23H28N6O9/c24-28-25-6-7-35-8-9-36-10-11-37-12-13-38-14-19(31)26-16-3-1-2-15-20(16)23(34)29(22(15)33)17-4-5-18(30)27-21(17)32/h1-3,17H,4-14H2,(H,26,31)(H,27,30,32)

InChI 密鑰

FGEDVKSXXCVRFL-UHFFFAOYSA-N

應用

Protein degrader builiding block Pomalidomide-PEG₄-Azide 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 azide for click chemistry with a 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 azide, 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

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

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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主要文件

Pomalidomide-PEG4-Azide

≥95%

About This Item

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属性

ligand

化驗

形狀

反應適用性

官能基

儲存溫度

SMILES 字串

InChI

InChI 密鑰

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-PEG₄-Azide