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Article

Discovery of JND3229 as a New EGFRC797S Mutant Inhibitor with In Vivo Monodrug Efficacy

8 Oct 2018

Abstract excerpt

EGFR C797S mutation inducing resistance against third generation EGFR inhibitor drugs is an emerging “unmet clinical need” for nonsmall cell lung cancer patients. The pyrimidopyrimidinone derivative JND3229 was identified as a new highly potent EGFR C797S inhibitor with single digit nM potency. It also exhibited good in vitro and in vivo monodrug anticancer efficacy in a xenograft mouse model of BaF3/EGFR...

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PMID: 30429956
DOI: 10.1021/acsmedchemlett.8b00373

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