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文件

921300

C5 Lenalidomide-pyrimidine-piperazine-PEG₁-NH₂ hydrochloride

Name: C5 Lenalidomide-pyrimidine-piperazine-PEG<SUB>1</SUB>-NH<SUB>2</SUB> hydrochloride
Brand: ALDRICH

≥95%

同義詞:

5-(4-(2-(2-Aminoethoxy)ethyl)piperazin-1-yl)-N-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)pyrimidine-2-carboxamide 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

經驗公式（希爾表示法）:

C₂₆H₃₂N₈O₅ · xHCl

分子量：:

536.58 (free base basis)

分類程式碼代碼:

12352101

NACRES:

NA.22

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Sigma-Aldrich

921327

C5 Lenalidomide-PEG₆-Butyl NH₂ hydrochloride

Sigma-Aldrich

911704

C5 Lenalidomine-C₃-NH₂ hydrochloride

Sigma-Aldrich

911755

C5 Lenalidomide-PEG₅-NH₂ hydrochloride

Sigma-Aldrich

919896

C5 Lenalidomide-dipiperazine-NH₂ hydrochloride

Sigma-Aldrich

911739

C5 Lenalidomide-PEG₁-NH₂ hydrochloride

Sigma-Aldrich

917729

C5 Lenalidomide-piperazine-pyridine-alkyne-NH₂ hydrochloride

Sigma-Aldrich

919969

C5 Lenalidomide-PEG₂-Butyl NH₂ hydrochloride

Sigma-Aldrich

920797

C5 Lenalidomide-pyridine-PEG₁-piperazine hydrochloride

Sigma-Aldrich

901504

Pomalidomide-PEG₃-CO₂H

Sigma-Aldrich

911690

C5 Lenalidomide

ligand

C5 Lenalidomide

品質等級

100

化驗

≥95%

形狀

(Powder or crystals or flakes or chunks)

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(C4=NC=C(N5CCN(CCOCCN)CC5)C=N4)=O)=CC=C31.Cl

應用

Protein degrader builiding block C5 Lenalidomide-pyrimidine-piperazine-PEG₁-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 linker with added rigidity, 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.

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

分析證明 (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

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

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

文章

針對蛋白質降解的降解器構件

Protein Degrader Building Blocks 是一系列交聯劑-E3 配體結合物，具有懸垂功能基團，可與目標配體共價連結。

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-pyrimidine-piperazine-PEG1-NH2 hydrochloride

≥95%

About This Item

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屬性

ligand

品質等級

化驗

形狀

反應適用性

官能基

儲存溫度

SMILES 字串

相關類別

描述

應用

其他說明

法律資訊

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安全資訊

儲存類別代碼

水污染物質分類（WGK）

閃點（°F）

閃點（°C）

文件

分析證明 (COA)

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C5 Lenalidomide-pyrimidine-piperazine-PEG₁-NH₂ hydrochloride