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Association details:
| Biomarker: | EGFR L858R + EGFR T790M |
|---|---|
| Cancer: | Non Small Cell Lung Cancer |
| Drug: | Xegafri (rociletinib) (EGFR inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
Synthesis and Fundamental Evaluation of Radioiodinated Rociletinib (CO-1686) as a Probe to Lung Cancer with L858R/T790M Mutations of Epidermal Growth Factor Receptor (EGFR)
Published date:
06/24/2020
Excerpt:
The selectivity of the tracer for detecting EGFR L858R/T790M was evaluated using three relevant non-small cell lung cancer (NSCLC) cell lines-H1975, H3255 and H441 overexpressing the dual mutation EGFR L858R/T790M, active mutant EGFR L858R and wild-type EGFR, respectively...In the cell uptake study, the radioactivity uptake of [125I]ICO1686 in H1975 was 101.52% dose/mg, whereas the uptakes in H3255 and H441 were 33.52 and 8.95% dose/mg, respectively. The uptake of [125I]ICO1686 in H1975 was greatly reduced to 45.61% dose/mg protein by treatment with excess CO-1686.
DOI:
10.3390/molecules25122914
