Crosslinker–E3 Ligase ligand conjugate

产品名称：

Pomalidomide-PEG₃-NH₂ hydrochloride
2-(2-(2-(2-Aminoethoxy)ethoxy)ethoxy)-N-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)acetamide hydrochloride
Protein degrader building block for PROTAC research
Crosslinker–E3 Ligase ligand conjugate
Template for synthesis of targeted protein degrader

产品介绍：

产品说明

应用

Protein degrader builiding block Pomalidomide-PEG₃-NH₂ (HCl salt) enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand and a PEGylated crosslinker with pendant amine for reactivity with a carboxyl group 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.

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

基本信息

经验(实验)分子式	C₂₁H₂₆N₄O₈ · xHCl
分子量	462.45 (free base basis)
NACRES	NA.22

产品性质

质量水平	100
测定	≥95%
形式	powder or crystals
运输	wet ice
储存温度	2-8℃
SMILES string	O=C(C(CC1)N(C2=O)C(C3=C2C=CC=C3NC(COCCOCCOCCN)=O)=O)NC1=O.Cl

安全信息

储存分类代码	13 - Non Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable

Pomalidomide-PEG3-NH2 hydrochloride

Pomalidomide-PEG₃-NH₂ hydrochloride