C5 Lenalidomine-C₆-NH₂ hydrochloride

C₂₀H₂₆N₄O₄ · xHCl

386.44 (free base basis)

Protein degrader builiding block C5 Lenalidomide-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 with alternative exit vector and an alkyl-chain 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.

Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation

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Small-Molecule PROTACS: New Approaches to Protein Degradation

Targeted Protein Degradation: from Chemical Biology to Drug Discovery

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

100

≥95%

powder or crystals

2-8℃

O=C1N(C2CCC(NC2=O)=O)CC3=CC(NC(CCCCCCN)=O)=CC=C31.Cl
O=C1N(C2CCC(NC2=O)=O)CC3=CC(NC(CCCCCCN)=O)=CC=C31.Cl

GHS08

Warning

H361d - H373

P201 - P308 + P313

Repr. 2 - STOT RE 2

Blood

11 - Combustible Solids

WGK 1