Discovery of STX-721, a Covalent, Potent, and Highly Mutant-Selective EGFR/HER2 Exon20 Insertion Inhibitor for the Treatment of Non-Small Cell Lung Cancer.

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Tác giả: Deanna R Borrelli, Natasja Brooijmans, Angel Guzman-Perez, Jack A Henderson, Brendan J Hilbert, Michael R Huff, Takahiro Ito, Erica L Jackson, Philip Jonsson, Brendon Ladd, Benjamin C Milgram, Erin L O'Hearn, Raymond A Pagliarini, Simon A Roberts, Sébastien Ronseaux, Darrin D Stuart, Weixue Wang

Ngôn ngữ: eng

Ký hiệu phân loại: 920.71 Men

Thông tin xuất bản: United States : Journal of medicinal chemistry , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 178138

After L858R and ex19del epidermal growth factor receptor (EGFR) mutations, ex20ins mutations are the third most common class of driver-mutations in non-small cell lung cancer (NSCLC). Unfortunately, first-, second-, and third-generation EGFR tyrosine kinase inhibitors (TKIs) are generally ineffective for ex20ins patients due to insufficient mutant activity and selectivity over wild-type EGFR, leading to dose-limiting toxicities. While significant advances in recent years have been made toward identifying potent EGFR ex20ins mutant inhibitors, mutant vs wild-type EGFR selectivity remains a significant challenge. STX-721 (
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