910449

Pomalidomide-PEG₂-butyl CO₂H

≥95%

• 别名: 7-(2-(2-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-2-oxoethoxy)ethoxy)heptanoic acid, Crosslinker−E3 ligase ligand conjugate, Pomalidomide conjugate, Pomalidomide-2-2-6-acid, Protein degrader building block for PROTAC^® research, Template for synthesis of targeted protein degrader
• 经验公式（希尔记法）: C₂₄H₂₉N₃O₉
• 分子量: 503.50
• MDL號碼: MFCD32669897
• 分類程式碼代碼: 12352101
• NACRES: NA.22

属性

• ligand: pomalidomide
• 化驗: ≥95%
• 形狀: powder
• 反應適用性: reactivity: amine reactive; reagent type: ligand-linker conjugate
• 官能基: carboxylic acid
• 儲存溫度: 2-8°C
• SMILES 字串: O=C(C(CC1)N(C2=O)C(C3=C2C=CC=C3NC(COCCOCCCCCCC(O)=O)=O)=O)NC1=O
• InChI: 1S/C24H29N3O9/c28-18-10-9-17(22(32)26-18)27-23(33)15-6-5-7-16(21(15)24(27)34)25-19(29)14-36-13-12-35-11-4-2-1-3-8-20(30)31/h5-7,17H,1-4,8-14H2,(H,25,29)(H,30,31)(H,26,28,32)
• InChI 密鑰: PTXYFBNBOJXGJO-UHFFFAOYSA-N

说明

應用

Protein degrader builiding block Pomalidomide-PEG₂-butyl CO₂H enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand, a linker with both hydrophobic and hydrophilic moieties, and a pendant carboxylic acid for reactivity with an amine 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 carboxyl group, 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

安全信息

• 象形圖: GHS08
• 訊號詞: Danger
• 危險聲明: H360D
• 防範說明: P201 - P202 - P280 - P308 + P313 - P405 - P501
• 危險分類: Repr. 1B
• 儲存類別代碼: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable