2230821-27-7

2230821-27-7 structure

Name: Gefitinib-based PROTAC 3
Chemical Name: Gefitinib-based PROTAC 3
CAS Number: 2230821-27-7
Molecular Formula: C₄₇H₅₇ClFN₇O₈S
Molecular Weight: 934.51
Catalog: Signaling Pathways JAK/STAT Signaling EGFR
Create Date: 2019-06-01 18:51:14
Modify Date: 2024-01-07 00:07:31
Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively[1].

Name	Gefitinib-based PROTAC 3

Description	Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> JAK/STAT Signaling >> EGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR Signaling Pathways >> PROTAC >> PROTAC
Target	EGFR:11.7 nM (DC50, HCC827(exon 19 del) cells) EGFR:22.3 nM (DC50, H3255 (L858R mutantion) cells) PROTAC
In Vitro	H3255 cells expressing L858R EGFR treated with Gefitinib-based PROTAC 3 (25 nM-10 μM; 24 hours), HCC827 cells expressing exon 19 del EGFR treated with Gefitinib-based PROTAC 3 (100 nM-10 μM; 24 hours), which enables the degradation of both exon-19 deletion EGFR as well as the mutant isoform containing the L858R activating point mutation, while sparing the WT EGFR[1]. Western Blot Analysis[1] Cell Line: HCC827 cells expressing exon 19 del EGFR; H3255 cells expressing L858R EGFR Concentration: 100 nM, 250 nM, 1 μM, 2.5 μM, 10 μM for HCC827 cells; 25 nM, 100 nM, 1 μM, 2.5 μM, 10 μM for H3255 cells Incubation Time: 24 hours Result: Degradation of both exon-19 deletion EGFR as well as the mutant isoform containing the L858R activating point mutation.
References	[1]. Burslem GM, et al. The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study. Cell Chem Biol. 2018 Jan 18;25(1):67-77.e3.