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2230821-27-7

2230821-27-7 structure
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
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.

Molecular Formula C47H57ClFN7O8S
Molecular Weight 934.51
Storage condition 2-8℃