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Key Documents

927732

Sigma-Aldrich

C5 Lenalidomide-difluoroPEG1-C4-piperazine Hydrochloride

≥95%

同義詞:

2-(2,2-Difluoro-3-(4-(piperazin-1-yl)butoxy)propoxy)-N-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)acetamide Hydrochloride

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About This Item

經驗公式(希爾表示法):
C26H35F2N5O6 · xHCl
分子量::
551.58 (free base basis)
NACRES:
NA.22

ligand

C5 Lenalidomide

品質等級

化驗

≥95%

形狀

powder

儲存溫度

2-8°C

SMILES 字串

O=C1N(C2CCC(NC2=O)=O)CC3=CC(NC(COCC(F)(F)COCCCCN4CCNCC4)=O)=CC=C31.Cl

應用

Protein degrader building block C5 Lenalidomide-difluoroPEG1-C4-piperazine Hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand, a fluorinated linker with both hydrophobic and hydrophilic moieties, 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 pendant amine, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.


Targeted Protein Degradation

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 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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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

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