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Association details:
| Biomarker: | EGFR T790M |
|---|---|
| Cancer: | Non Small Cell Lung Cancer |
| Drug: | Compound 6a (EGFR inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
Novel third-generation pyrimidines-based EGFR tyrosine kinase inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer
Published date:
03/16/2022
Excerpt:
Compound 6a showed good inhibitory activity against EGFR mutant cells with an IC50 value of 0.0022 ± 0.001 μM and was approximately 1730-fold less potent against EGFR WT cells (IC50: 4.499 ± 0.057 μM)….Additionally, in vivo studies confirmed that 6a suppressed tumor growth in an H1975 xenograft model (25 mg/kg/d, TGI: 90.24%). Overall, these results suggest that 6a could be a promising lead compound for overcoming the clinical EGFR T790M resistance of patients with non-small-cell lung cancers (NSCLCs).
DOI:
10.1016/j.bioorg.2022.105743
