产品说明
应用
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.
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
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 | C17H20N4O5 · xHCl |
分子量 | 360.36 (free base basis) |
产品性质
质量水平 | 100 |
测定 | ≥95% |
形式 | powder |
储存温度 | 2-8℃ |
SMILES string | O=C1N(C2CCC(NC2=O)=O)CC3=CC(NC(COCCN)=O)=CC=C31.Cl O=C1N(C2CCC(NC2=O)=O)CC3=CC(NC(COCCN)=O)=CC=C31.Cl |
安全信息
象形图 | |
警示用语: | Warning |
危险声明 | H361d - H373 |
预防措施声明 | P201 - P308 + P313 |
危险分类 | Repr. 2 - STOT RE 2 |
靶器官 | Blood |
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 1 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |