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STX-721, a Covalent EGFR/HER2 Exon 20 Inhibitor, Utilizes Exon 20-Mutant Dynamic Protein States and Achieves Unique Mutant Selectivity Across Human Cancer Models

Pagliarini RA, Henderson JA, Milgram BC, … Stuart DD · Clin Cancer Res 2025 · Clin Cancer Res 31(14):3002-3018

EGFR/HER2 exon 20 mutants Tyrosine kinase Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profilingMechanism & structural biology PhosphoSens

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