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BDTX-189, a novel tyrosine kinase inhibitor, inhibits cell activity via ERK and AKT pathways in the EGFR C797S triple mutant cells.

Chemico-biological interactions - 25 May 2024

Wang Rui, Cui Wenrui, Li Lanxin, Wei Xiangkai, Chu Chunhong, Zhang Guoliang, Liu Chenxue, Xu Huixia, Liu Chenyang, Wang Ke, Li Yanming, An Lei

Abstract excerpt

The tertiary mutation C797S in the structural domain of the EGFR kinase is a common cause of resistance to third-generation EGFR tyrosine kinase inhibitors (TKIs). In this study, we used a potent, selective and irreversible inhibitor, BDTX-189, to target EGFR C797S triple mutant cells for cell activity. The study constructed the H1975-C797S (EGFR L858R/T790 M/C797S) cell line using the CRISPR/Cas9 method and...

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PMID: 38710274
DOI: 10.1016/j.cbi.2024.111033

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