Journal: JTO Clinical and Research Reports

Article Title: The Impact of On-Target Resistance Mediated by EGFR-T790M or EGFR-C797S on EGFR Exon 20 Insertion Mutation Active Tyrosine Kinase Inhibitors

doi: 10.1016/j.jtocrr.2023.100614

Figure Lengend Snippet: Mechanisms of Reported On-Target and Off-Target Resistance to EGFR Exon 20 Insertion Mutation Active TKIs

Article Snippet: Furmonertinib (MedChemExpress) was mixed with DMSO at 5 mM immediately before each experiment.

Techniques: Mutagenesis, Amplification

Journal: JTO Clinical and Research Reports

Article Title: The Impact of On-Target Resistance Mediated by EGFR-T790M or EGFR-C797S on EGFR Exon 20 Insertion Mutation Active Tyrosine Kinase Inhibitors

doi: 10.1016/j.jtocrr.2023.100614

Figure Lengend Snippet: The impact of EGFR-T790M or EGFR-C797S in the sensitivity of different EGFR TKIs in the background of different types of EGFR mutants. ( A ) Therapeutic window of different EGFR TKIs to EGFR mutants. Cells were plated at a density of 10,000 cells per well (96-well plates) and grown over 3 days after treatment. IC 50 of EGFR mutants compared with EGFR-WT is plotted with three separate experiments used to generate IC 50 . Values below zero (0) indicate sensitivity, whereas values above 0 indicate resistance to EGFR TKIs. The therapeutic window of Ba/F3 cells with EGFR mutants (A767_V769dupASV, D770_N771insSVD, V773_C774insH, delE746_A750, L858R in the presence or absence of EGFR-T790M or EGFR-C797S) were plotted for each EGFR TKI (osimertinib, poziotinib, mobocertinib, zipalertinib, furmonertinib, sunvozertinib). ( B ) Dose-response proliferation assays (percent viability) for cell lines harboring EGFR-D770_N771insSVD in the absence or presence of EGFR-T790M or EGFR-C797S after exposure to increasing concentrations of zipalertinib, furmonertinib, and sunvozertinib. Three separate experiments were used to generate IC 50 , and SDs are depicted in vertical bars. IC 50 , 50% inhibitory concentration; pEGFR, phosphorylated EGFR; TKI, tyrosine kinase inhibitor; WT, wild type.

Article Snippet: Furmonertinib (MedChemExpress) was mixed with DMSO at 5 mM immediately before each experiment.

Techniques: Concentration Assay

Journal: Lung Cancer: Targets and Therapy

Article Title: Spotlight on Furmonertinib (Alflutinib, AST2818). The Swiss Army Knife (del19, L858R, T790M, Exon 20 Insertions, “uncommon-G719X, S768I, L861Q”) Among the Third-Generation EGFR TKIs?

doi: 10.2147/LCTT.S385437

Figure Lengend Snippet: Comparison of the structure of furmonertinib and osimertinib.

Article Snippet: Furmonertinib (AST2818, Alflutinib) is manufactured by Shanghai Allist Pharmaceuticals Co., Ltd. in Shanghai, China.

Techniques: Comparison

Journal: Lung Cancer: Targets and Therapy

Article Title: Spotlight on Furmonertinib (Alflutinib, AST2818). The Swiss Army Knife (del19, L858R, T790M, Exon 20 Insertions, “uncommon-G719X, S768I, L861Q”) Among the Third-Generation EGFR TKIs?

doi: 10.2147/LCTT.S385437

Figure Lengend Snippet: Comparison of Incidence of QTc Prolongation Between Furmonertinib and Osimertinib

Article Snippet: Furmonertinib (AST2818, Alflutinib) is manufactured by Shanghai Allist Pharmaceuticals Co., Ltd. in Shanghai, China.

Techniques: Comparison

Journal: The Innovation

Article Title: Acquired resistance to third-generation EGFR-TKIs and emerging next-generation EGFR inhibitors

doi: 10.1016/j.xinn.2021.100103

Figure Lengend Snippet: Clinical progress of the third-generation EGFR-TKIs

Article Snippet: Alflutinib , phase III , Allist Pharma , NSCLC , NCT03787992 , Wang and Adjei .

Techniques: Clinical Proteomics