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DRUG:

14aj

i
Other names: 14aj, compound 14aj
Company:
Nankai University School of medicine
Drug class:
EGFR inhibitor
Related drugs:
over2years
Discovery and structural optimization of potent epidermal growth factor receptor (EGFR) inhibitors against L858R/T790M/C797S resistance mutation for lung cancer treatment. (PubMed, Eur J Med Chem)
The C797S mutation in EGFR is a leading mechanism of clinically acquired resistance against osimertinib for non-small cell lung cancer (NSCLC). In vivo xenograft mouse model, oral administration of compound 14aj led to significant tumor regression without obvious toxicity. In addition, this compound showed good pharmacokinetics.
Journal
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L858R • EGFR T790M • EGFR C797S
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Tagrisso (osimertinib) • 14aj