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文件

921327

C5 Lenalidomide-PEG₆-Butyl NH₂ hydrochloride

Name: C5 Lenalidomide-PEG<SUB>6</SUB>-Butyl NH<SUB>2</SUB> hydrochloride
Brand: ALDRICH

≥95%

别名:

24-Amino-N-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)-3,6,9,12,15,18-hexaoxatetracosanamide hydrochloride, 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）:

C₃₁H₄₈N₄O₁₀ · xHCl

分子量:

636.73 (free base basis)

NACRES:

NA.22

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Slide 1 of 10

1 of 10

Sigma-Aldrich

911704

C5 Lenalidomine-C₃-NH₂ hydrochloride

Sigma-Aldrich

794333

聚 [2,6′]-4,8-二（5-乙基己基噻吩）苯并 [1,2-b;3,3-b] 二噻吩 ] {3-氟-2 [（2-乙基己基）羰基] 噻吩 [3,4-b] 噻吩二基 }）

Sigma-Aldrich

CIX001

ComInnex IAP Ligand Library

Sigma-Aldrich

920797

C5 Lenalidomide-pyridine-PEG₁-piperazine hydrochloride

Sigma-Aldrich

917206

A1V2PF1-NHEt-C₁₀-NH₂

Sigma-Aldrich

923931

Pomalidomide-4-piperidine-C₁-piperazine hydrochloride

Sigma-Aldrich

923443

PhMPhos

Sigma-Aldrich

445703

聚(3-己基噻吩-2,5-二基)

Sigma-Aldrich

660485

3,4-亚丙基二氧噻吩

Sigma-Aldrich

920827

(S,R,S)-AHPC-methylamino-PEG₁-NH₂ hydrochloride

ligand

C5 Lenalidomide

品質等級

100

化驗

≥95%

形狀

powder or crystals

反應適用性

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

官能基

amine

儲存溫度

2-8°C

SMILES 字串

O=C1N(C2CCC(NC2=O)=O)CC3=CC(NC(COCCOCCOCCOCCOCCOCCCCCCN)=O)=CC=C31.Cl

應用

Protein degrader builiding block C5 Lenalidomide-PEG6-Butyl NH2 hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand with alternative exit vector, a PEGylated linker, and a pendant amine for reactivity with a carboxylic acid 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 terminal amine, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

Technology Spotlight:Degrader Building Blocks for Targeted Protein Degradation

Portal:Building PROTAC^® Degraders for Targeted Protein Degradation

其他說明

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

分析证书(COA)

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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

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

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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C5 Lenalidomide-PEG6-Butyl NH2 hydrochloride

≥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

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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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C5 Lenalidomide-PEG₆-Butyl NH₂ hydrochloride