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Key Documents

911739

Sigma-Aldrich

C5 Lenalidomide-PEG1-NH2 hydrochloride

≥95%

同義詞:

2-(2-Aminoethoxy)-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):
C17H20N4O5 · xHCl
分子量::
360.36 (free base basis)
分類程式碼代碼:
12352101
NACRES:
NA.22

ligand

C5 Lenalidomide

品質等級

化驗

≥95%

形狀

powder

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

應用

Protein degrader builiding block C5 Lenalidomide-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 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)

法律資訊

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

相關產品

產品號碼
描述
訂價

象形圖

Health hazard

訊號詞

Warning

危險聲明

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


分析證明 (COA)

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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

文章

Partial PROTACs are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

Partial PROTACs are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

Partial PROTACs are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

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 (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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