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Anti-cancer composition with synergistic effect

A technology of synergistic effect and composition, which can be used in medical preparations containing active ingredients, drug combinations, anti-tumor drugs, etc. The effect of reducing the risk of treatment

Active Publication Date: 2018-06-22
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The 2-position (containing N-arylpiperazine structure) substituted quinazoline derivatives C2 and C17 have a strong affinity with D1DR, but there are no reports on the effect of these compounds on tumors

Method used

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  • Anti-cancer composition with synergistic effect
  • Anti-cancer composition with synergistic effect
  • Anti-cancer composition with synergistic effect

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] C2, C17 and SN alone inhibit the proliferation of pancreatic cancer cells

[0031] Take logarithmic growth phase cells, digest with 0.25% trypsin-0.53mmol / L EDTA solution, centrifuge, resuspend and count. Both SW1990 cells and PANC-1 cells were seeded on 96-well cell culture plates at 6000 cells / well. After culturing for 24 hours, the drug was administered. For SW1990 cells, the final concentration of C2 single-drug administration group is: 0.1, 1, 2.5, 5, 10, 15, 50, 100μM; for PANC-1 cells, the final concentration of C2 single-drug administration group is: 0.1, 1, 2, 6, 8, 10, 20, 50μM. In the two cell lines, the final concentration of C17 single-drug administration group was: 1, 5, 10, 15, 20, 25, 30, 50, 100 μM. In the two cell lines, the final concentration of the SN single-drug administration group was: 0.1, 0.5, 1, 5, 7, 10, 15, 50, 100 μM. Each group has 6 parallel holes. Continue to incubate for 48h. After the incubation, the medium was discarded, and 100 μ...

Embodiment 2

[0035] Inhibitory effect of C2 combined with SN on the proliferation of human pancreatic cancer cells

[0036] Take logarithmic growth phase cells, digest with 0.25% trypsin-0.53mmol / L EDTA solution, centrifuge, resuspend and count. Both SW1990 cells and PANC-1 cells were seeded on 96-well cell culture plates at 6000 cells / well. After culturing for 24 hours, the drug was administered. For the three parallel 96-well plates of SW990 cells, the concentrations of SN are 0, 1, and 5 μmol / L. For the four parallel 96-well plates of PANC-1 cells, the concentrations of SN are 0, 2, 5, 10μmol / L, and in each 96-well plate, the concentration of C2 is set to 0, 1, 2, 4μmol / L, and each group has 6 parallel wells. Continue to incubate for 48h. The absorbance of each well at 540 nm was measured by the SRB method. The method reported in the literature was used to calculate the size of the CI (combination index, CI). Calculate the theoretical absorbance of the combined administration group a...

Embodiment 3

[0041] Inhibitory effect of C17 combined with SN on the proliferation of human pancreatic cancer cells

[0042] Take logarithmic growth phase cells, digest with 0.25% trypsin-0.53mmol / L EDTA solution, centrifuge, resuspend and count. Both SW1990 cells and PANC-1 cells were seeded on 96-well cell culture plates at 6000 cells / well. After culturing for 24 hours, the drug was administered. For the four parallel 96-well plates of two kinds of cells, the concentration of C17 is 0, 1, 4, and 10 μmol / L. In each 96-well plate, the concentration of SN is set to 0, 1, 2, and 5 μmol / L. L, each group has 6 parallel holes. Continue to incubate for 48h. The absorbance of each well at 540 nm was measured by the SRB method. The method reported in the literature was used to calculate the size of the CI (combination index, CI). Calculate the theoretical absorbance of the combined administration group according to formula 3.1, and the ratio of the measured absorbance to the theoretical value i...

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Abstract

The invention relates to an anti-cancer composition with a synergistic effect. The composition comprises at least one kind of VEGF / VEGFR inhibitor with effective dose and 2-position (containing an N-aryl piperazine structure) substituted quinazoline derivative composition. The composition can significantly inhibit the growth of tumour cells and reduce the using amount of anti-cancer drugs, the treating risk and cost, and the composition has wide application prospect.

Description

Technical field [0001] The invention relates to an anticancer composition with synergistic effect, a preparation method and application thereof. Background technique [0002] Cancer, also known as malignant tumor, is caused by abnormal cell proliferation. These abnormally proliferated cells invade other parts of the body. The current traditional methods of treating cancer include surgery, radiotherapy, chemotherapy, immunotherapy, gene therapy, etc. Because the reasons that affect the occurrence and development of tumors are very complex, and drug resistance and tumor recurrence are prone to occur during the treatment process, tumor treatment is more difficult. [0003] In the entire tumor tissue, only a small part of tumor cells are tumorigenic, that is, cancer stem cells (Cancerstem cell, CSC). The production of CSC is closely related to the self-renewal ability of cancer cells, resistance to traditional chemotherapy, and tumor recurrence and metastasis. Sunitinib (SN) is a mu...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K31/517A61K31/404A61P35/00
CPCA61K31/404A61K31/517A61K45/06A61K2300/00
Inventor 周田彦陈国术苏红薛子溪冯瑶瑶
Owner PEKING UNIV
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