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920738

Pomalidomide-C9-NH2 hydrochloride

Synonyme(s) :

4-((9-Aminononyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione hydrochloride, Crosslinker-E3 Ligase ligand conjugate, Protein degrader building block for PROTAC® research, Template for synthesis of targeted protein degrader

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A propos de cet article

Formule empirique (notation de Hill) :
C22H31ClN4O4
Numéro CAS:
Poids moléculaire :
450.96
MDL number:
UNSPSC Code:
12352101
NACRES:
NA.22
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ligand

pomalidomide

Quality Level

form

crystals

reaction suitability

reactivity: carboxyl reactive, reagent type: ligand-linker conjugate

functional group

amine

storage temp.

−20°C

SMILES string

O=C(C(CC1)N(C2=O)C(C3=C2C=CC=C3NCCCCCCCCCN)=O)NC1=O.Cl

InChI key

NCVSGGBARHERSU-UHFFFAOYSA-N

Application

Protein degrader builiding block Pomalidomide-C9-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, a rigid linker, 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.

Legal Information

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


pictograms

Health hazard

signalword

Danger

hcodes

Hazard Classifications

Repr. 1B

Classe de stockage

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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Daniel P Bondeson et al.
Annual review of pharmacology and toxicology, 57, 107-123 (2016-10-13)
Protein homeostasis networks are highly regulated systems responsible for maintaining the health and productivity of cells. Whereas therapeutics have been developed to disrupt protein homeostasis, more recently identified techniques have been used to repurpose homeostatic networks to effect degradation of



Numéro d'article de commerce international

RéférenceGTIN
920738-50MG04065266033397