920789

Pomalidomide-pyridine-PEG₁-piperazine hydrochloride

• Szinonimák: N-(2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)-2-(6-(3-(piperazin-1-yl)propoxy)pyridin-3-yl)acetamide hydrochloride, Crosslinker−E3 Ligase ligand conjugate, Protein degrader building block for PROTAC^® research, Template for synthesis of targeted protein degrader
• Tapasztalati képlet (Hill-képlet): C₂₇H₃₀N₆O₆ · xHCl
• Molekulatömeg: 534.56 (free base basis)
• MDL-szám: MFCD34549907
• UNSPSC kód: 12352200
• NACRES: NA.22

Tulajdonságok

• ligand: pomalidomide
• Minőségi szint: 100
• Forma: powder or crystals
• reakcióalkalmasság: reactivity: carboxyl reactive; reagent type: ligand-linker conjugate
• funkcionális csoport: amine
• tárolási hőmérséklet: 2-8°C
• SMILES string: O=C(N(C1CCC(NC1=O)=O)C2=O)C3=C2C=CC=C3NC(CC4=CC=C(OCCCN5CCNCC5)N=C4)=O.Cl
• InChI: 1S/C27H30N6O6.ClH/c34-21-7-6-20(25(36)31-21)33-26(37)18-3-1-4-19(24(18)27(33)38)30-22(35)15-17-5-8-23(29-16-17)39-14-2-11-32-12-9-28-10-13-32;/h1,3-5,8,16,20,28H,2,6-7,9-15H2,(H,30,35)(H,31,34,36);1H
• Nemzetközi kémiai azonosító kulcs: NQWAQGYTEGUDBW-UHFFFAOYSA-N

Leírás

Alkalmazás

Protein degrader building block Pomalidomide-pyridine-PEG₁-piperazine hydrochloride 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 added rigidity, and a pendant amine for reactivity with a carboxylic 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 pendant amine, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

Egyéb megjegyzések

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

Jogi információk

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

Biztonsági adatok

• Tárolási osztály kódja: 11 - Combustible Solids
• WGK: WGK 3
• Lobbanási pont (F): Not applicable
• Lobbanási pont (C): Not applicable