A PROTAC comprised of gefitinib linked to VHL ligand 1; induces degradation of EGFR containing the activating mutation L858R or an exon 19 deletion (DC50s = 22.3 and 11.7 nM

Gefitinib-based PROTAC 3 – 5 mg

Brand:
Cayman
CAS:
2230821-27-7
Storage:
-20
UN-No:
Non-Hazardous - /

Gefitinib-based PROTAC 3 is a proteolysis-targeting chimera (PROTAC) comprised of the EGF receptor (EGFR) inhibitor gefitinib (Item No. 13166) linked to the von Hippel-Lindau (VHL) E3 ubiquitin ligase ligand VHL ligand 1 (Item No. 21591).{52051} In cell-based assays, gefitinib-based PROTAC 3 induces degradation of EGFR containing the activating mutation L858R or an exon 19 deletion with half-maximal degradation (DC50) values of 22.3 and 11.7 nM, respectively, but does not induce degradation of wild-type EGFR at concentrations up to 10 μM.  

 

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SKU: 28597 - 5 mg Category:

Description

A PROTAC comprised of gefitinib linked to VHL ligand 1; induces degradation of EGFR containing the activating mutation L858R or an exon 19 deletion (DC50s = 22.3 and 11.7 nM, respectively) but does not induce degradation of wild-type EGFR at ≤10 μM in cell-based assays

Formal name: (2S,4R)-1-((S)-2-(3-(2-((5-((4-((3-chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)pentyl)oxy)ethoxy)propanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

Synonyms:  Gefitinib-based Proteolysis-targeting Chimera 3

Molecular weight: 934.5

CAS: 2230821-27-7

Purity: ≥98%

Formulation: A crystalline solid

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