Gefitinib-based PROTAC 3

• CAT Number: I019173
• CAS Number: 2230821-27-7
• Molecular Formula: C₄₇H₅₇ClFN₇O₈S
• Molecular Weight: 934.51
• Purity: ≥95%
• Target: Protein Tyrosine Kinase/RTK

Gefitinib-based PROTAC 3 (CAT: I019173) is a cutting-edge molecular tool designed to harness the principles of proteolysis-targeting chimeras (PROTACs) for targeted protein degradation. By ingeniously combining an EGFR binding moiety with a Von Hippel-Lindau (VHL) ligand through a specialized linker, this innovative compound demonstrates its remarkable ability to induce degradation of the epidermal growth factor receptor (EGFR). In HCC827 cells harboring the exon 19 deletion mutation, Gefitinib-based PROTAC 3 achieves a compelling DC50 of 11.7 nM, while in H3255 cells carrying the L858R mutation, it exhibits an impressive DC50 of 22.3 nM.

Reference

[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.