EMI1 (ChemBridge 5213777) is a call penetrant and potent inhibitor of EGFR signaling in EGFR L858R/T790M/C797S and ex19del/T790M/C797S triple mutants associated with drug-resistant NSCLC. Additionally, EMI1 potently depolymerized interphase microtubules, disrupts spindle formation and induced mitotic block in PC9 EGFR ex19del/T790M/C797S cells. EMI1 exhibits potent anti-proliferative activity against various cancer cell lines.
call penetrant and potent inhibitor of EGFR signaling in EGFR L858R/T790M/C797S triple mutants associated with drug-resistant NSCLC
Microtubules are a proven target for anticancer drug development because they are critical for mitotic spindle formation and the separation of chromosomes at mitosis. We here report a novel synthetic microtubule inhibitor 7-diethylamino-3(2'-benzoxazolyl)-coumarin (DBC). DBC causes destabilization of microtubules, leading
Nature chemical biology, 16(5), 577-586 (2020-02-26)
Receptor tyrosine kinases (RTKs) are transmembrane receptors of great clinical interest due to their role in disease. Historically, therapeutics targeting RTKs have been identified using in vitro kinase assays. Due to frequent development of drug resistance, however, there is a
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