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安全和法规

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%

别名:

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

经验公式（希尔记法）:

C₂₆H₃₂N₈O₅ · xHCl

分子量:

536.58 (free base basis)

MDL编号:

MFCD34549913

UNSPSC代码:

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

911747

C5 Lenalidomide-PEG₃-NH₂ hydrochloride

Sigma-Aldrich

918350

C5 Lenalidomide-alkyne-piperidine 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

ligand

C5 Lenalidomide

质量水平

100

方案

≥95%

表单

(Powder or crystals or flakes or chunks)

反应适用性

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

官能团

amine

储存温度

2-8°C

SMILES字符串

O=C1N(C2CCC(NC2=O)=O)CC3=CC(NC(C4=NC=C(N5CCN(CCOCCN)CC5)C=N4)=O)=CC=C31.Cl

InChI

1S/C26H32N8O5.ClH/c27-5-11-39-12-10-32-6-8-33(9-7-32)19-14-28-23(29-15-19)25(37)30-18-1-2-20-17(13-18)16-34(26(20)38)21-3-4-22(35)31-24(21)36;/h1-2,13-15,21H,3-12,16,27H2,(H,30,37)(H,31,35,36);1H

InChI key

VEHCGTYYGZOLLK-UHFFFAOYSA-N

应用

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

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

新产品

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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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

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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C5 Lenalidomide-pyrimidine-piperazine-PEG1-NH2 hydrochloride

≥95%

About This Item

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属性

ligand

质量水平

方案

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

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其他说明

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储存分类代码

WGK

闪点(°F)

闪点(°C)

法规信息

文件

分析证书(COA)

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C5 Lenalidomide-pyrimidine-piperazine-PEG₁-NH₂ hydrochloride