Gefitinib-based PROTAC 3

A PROTAC that drives mutant EGFR degradation

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货号: ajci23260
CAS: 2230821-27-7
别名: Gefitinib-based Proteolysis-targeting Chimera 3
分子式: C47H57ClFN7O8S
分子量: 934.522
纯度: >98%
溶解度: DMF: 25 mg/ml,DMF:PBS (pH 7.2) (1:3): 0.25 mg/ml,DMSO: 16 mg/ml,Ethanol: 10 mg/ml
储存: 4°C, away from moisture and light
库存: 现货

Background

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].

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].

参考文献:
[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.