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911747

Sigma-Aldrich

C5 Lenalidomide-PEG3-NH2 hydrochloride

≥95%

同義詞:

2-(2-(2-(2-Aminoethoxy)ethoxy)ethoxy)-N-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)acetamide hydrochloride, C5 Lenalidomide conjugate, 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）:
C21H28N4O7 · xHCl
分子量：:
448.47 (free base basis)
分類程式碼代碼:
12352101

ligand

C5 Lenalidomide

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(COCCOCCOCCN)=O)=CC=C31.Cl

應用

Protein degrader builiding block C5 Lenalidomide-PEG3-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 and a PEGylated crosslinker with pendant amine for reactivity with an acid on the target warhead. Because even slight alterations in ligands, warheads, 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.

Automate your CRBN-PEG based PROTACs with Synple Automated Synthesis Platform (SYNPLE-SC002)

其他說明

Degrader Building Blocks for Targeted Protein Degradation.

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

法律資訊

PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license

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象形圖

Health hazard
GHS08

訊號詞

Warning

危險聲明

H361d,H373

防範說明

P201 - P308 + P313

危險分類

Repr. 2 - STOT RE 2

標靶器官

Blood

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 1

閃點（°F）

Not applicable

閃點（°C）

Not applicable

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分析證明 (COA)

Lot/Batch Number
MKCM1378

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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
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
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

文章

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.

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.

相關內容

Targeted Protein Degradation

Targeted protein degradation (TPD) is an emerging drug discovery strategy that uses small-molecules, such as proteolysis-targeting chimeras (PROTACs), to eradicate targeted proteins linked to disease from cells.

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