Application of bis-indole compound FGFC1 in preparation of medicaments resistant to non-small cell lung cancer

A technology for non-small cell lung cancer and bisindole compound, which is applied in the application field of bisindole compound and the preparation of anti-non-small cell lung cancer drugs, and can solve the problems of limiting therapeutic efficacy and the like

Active Publication Date: 2019-08-23
SHANGHAI OCEAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are three generations of EGFR-TKIs currently on the market in China, and only the third-generation inhibitor Osimertinib has higher activity and selectivity for EGFR T790M mutation, which can alleviate the inhibition of wild-type EGFR. Toxic and side effects, however, the problem of acquired drug resistance still exists during clinical treatment, which limits the efficacy of treatment

Method used

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  • Application of bis-indole compound FGFC1 in preparation of medicaments resistant to non-small cell lung cancer
  • Application of bis-indole compound FGFC1 in preparation of medicaments resistant to non-small cell lung cancer
  • Application of bis-indole compound FGFC1 in preparation of medicaments resistant to non-small cell lung cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Inhibitory effect of FGFC1 on proliferation of cell lines of different tumor types.

[0031] (1) Cell inoculation: Four tumor cell lines (HCT116, HeLa, PC9 and MCF7) in the exponential growth phase were digested respectively, and suspensions were prepared with RPMI1640 or DMEM medium containing 10% calf serum. Tumor cells were seeded at 1×10 5 cells / mL inoculated in 96-well culture plate, add 100 μL to each well, at 37°C, CO 2 Cultivate in the incubator for 24h.

[0032] (2) Dosing: the compound to be tested was prepared into a stock solution with a certain concentration by adding DMSO, and then prepared into 5 μmol / L and 50 μmol / L solutions with RMPI1640 or DMEM medium containing 10% calf serum, and inoculated in 96 In a well-plated cell culture plate, set up three parallel wells for each concentration, at 37°C, 5% CO 2 Cultivate in the incubator for 48h. The control group was treated with DMSO, without adding drugs, and continued to culture for 48 hours. The chang...

Embodiment 2

[0036] The results of morphological changes of non-small cell lung cancer lines containing different driver genes treated with different concentrations of FGFC1 for the same time.

[0037] (1) Inoculated cells: respectively digest non-small cell lung cancer cell lines in exponential growth phase containing different driver genes: EGFR sensitive mutation PC9 (ex19del), EGFR primary resistance mutation H1975 (L858R / T790M), EGFR wild type A549 (KRAS mutation), H1299 (NRAS mutation). Suspension was made with RPMI1640 or DMEM medium containing 10% calf serum. The tumor cells were seeded with a cell number of 0.5×10 5 cells / mL inoculated in 12-well culture plate, add 2 mL to each well, at 37°C, CO 2 Cultivate in the incubator for 24h.

[0038] (2) Dosing: the compound to be tested was prepared into a stock solution with a certain concentration by adding DMSO, and then prepared into 5 μmol / L and 50 μmol / L solutions with RMPI1640 or DMEM medium containing 10% calf serum, and inoculat...

Embodiment 3

[0041] Inhibitory effect of FGFC1 on non-small cell lung cancer cell lines harboring different driver genes.

[0042] (1) Inoculated cells: respectively digest non-small cell lung cancer cell lines in exponential growth phase containing different driver genes: EGFR sensitive mutation PC9 (ex19del), EGFR primary resistance mutation H1975 (L858R / T790M), EGFR wild type A549 (KRAS mutation), H1299 (NRAS mutation). Suspension was made with RPMI1640 or DMEM medium containing 10% calf serum. Tumor cells were seeded at 1×10 5 cells / mL inoculated in 96-well culture plate, add 100 μL to each well, at 37°C, CO 2 Cultivate in the incubator for 24h.

[0043] (2) Dosing: the compound to be tested was prepared into a stock solution with a certain concentration by adding DMSO, and then prepared into 0.01, 0.1, 1, 2, 5, 10, 20 respectively with RMPI1640 or DMEM medium containing 10% calf serum , 40, 80, and 100 μmol / L solutions, inoculated in 96-well cell culture plates, and set up three p...

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Abstract

The invention belongs to the field of medicine preparation and particularly relates to application of a bis-indole compound FGFC1 in preparation of medicaments resistant to non-small cell lung cancer.The medicaments resistant to non-small cell lung cancer are EGFR-targeted medicaments resistant to human non-small cell lung cancer. EGFR sensitive and drug-resistant mutant cell lines are PC9 and H1975. The medicaments resistant to non-small cell lung cancer are at least made in one preparation form of tablets, capsules, granules, drop pills, suspensions, syrups, enteric preparations, emulsion suspensions and injections. The bis-indole compound FGFC1 not only has the potential of being developed into a new generation of the EGFR-targeted medicaments resistant to non-small-cell lung cancer but also has a potential application value in the fields of targeting medicaments, probe design and fluorescent biomarkers of non-small-cell lung cancer.

Description

technical field [0001] The invention belongs to the field of medicine preparation, and particularly relates to the application of bisindole compound FGFC1 in the preparation of anti-non-small cell lung cancer drugs. Background technique [0002] Cancer, as one of the diseases with a high incidence rate in the world, is constantly invading people's lives. Among them, lung cancer has become one of the most common fatal malignant tumors in the world, and its morbidity and mortality rank first among malignant tumors. In 2018, more than 1.8 million people died of lung cancer, and the death rate accounted for 18.4% of all cancer deaths, ranking first. Non-small cell lung cancer (NSCLC) accounts for 80%-85% of the total incidence of lung cancer. It is often diagnosed in the middle and advanced stages. Radiotherapy and chemotherapy are the main treatment methods, but the failure rate of clinical treatment is high, and the five-year survival rate is high. low rate. [0003] Natura...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/404A61P35/00
CPCA61K31/404A61P35/00
Inventor 刘宁吴文惠炎士珂董庆丰包斌郭锐华党璐童
Owner SHANGHAI OCEAN UNIV
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