产品说明

应用

Protein degrader building block Pomalidomide-C₆-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 and an alkyl-chain crosslinker with pendant amine for reactivity with an 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 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

Proteolysis Targeting Chimeras for the Selective Degradation of Mcl-1/Bcl-2 Derived from Nonselective Target Binding Ligands

Chemoselective Synthesis of Lenalidomide-Based PROTAC Library Using Alkylation Reaction

Identification of New Small-Molecule Inducers of Estrogen-related Receptor α (ERRα) Degradation

Discovery of MD-224 as a First-in-Class, Highly Potent and Efficacious PROTAC MDM2 Degrader Capable of Achieving Complete and Durable Tumor Regression

法律信息

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

基本信息

产品性质

安全信息

象形图
警示用语：	Danger
危险声明	H360D
预防措施声明	P201 - P308 + P313
危险分类	Repr. 1B
储存分类代码	6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable