36 results about "EGFR L858R" patented technology

The invention discloses a method for detecting mutation rate of lung cancer mutation sites. The method comprises the steps that (1) extraction of cfDNA is performed on a plasma sample of peripheral blood of a lung cancer patient to obtain a cfDNA extract; (2) for a lung cancer-associated EGFR L858R site, a first mutant detection probe (the sequence is SEQ ID NO:5) and a first wild type detection probe (the sequence is SEQ ID NO: 6), a first primer (the sequence is SEQ ID NO: 1) and a second primer (the sequence is SEQ ID NO: 2) are designed, and for a lung cancer-associated EGFR 19 exon deletion site, a second mutant detection probe (the sequence is SEQ ID NO: 7) and a second wild type detection probe (the sequence is SEQ ID NO: 8), a third primer (the sequence is SEQ ID NO: 3) and a fourth primer (the sequence is SEQ ID NO: 4) are designed; (3) the cfDNA extract is used as a template for ddPCR detection to obtain an amplification product containing a sensitive mutation site; (4) dataanalysis is performed on the amplification product to obtain the mutation rate of the EGFR sensitive mutation L858R and 19 Del. Thereby, the mutation rates of the EGFR sensitive mutation L858R and 19Del can be obtained sensitively.

The invention discloses pyrimidotricyclic compounds or pyrimidotetracyclic compounds having a structure represented by the formula (I), (II) or (III), pharmaceutically-acceptable salts, stereoisomers, or prodrug molecules. The compounds can inhibit various tumor cells, and especially, the compounds can selectively act on lung cancer cells of EGFR L858R / T790 and EGFR E745 A750 / T790M. Compared to wild type cancer cells, the IC50 of the compounds is 10 times, 100 times or even 1000 times higher. The compounds are a novel protein kinase inhibitor, which can overcome the drug resistance of EGFR-TKI and has selectivity.

The present application provides a compound of Formula (I) as an inhibitor against wild-type EGFR and / or mutant EGFR, which may be used for treating human non-small cell lung cancer individually or in combination with other therapeutic agent(s). The compound of Formula (I) of the present application may be used for treating patients of drug-resistant human non-small cell lung cancer harboring wild-type EGFR and / or EGFR T790M mutation and / or EGFR L858R mutation and / or EGFR delE746_A750 mutation.