Application of 4-[6-(4-isopropoxypheny) pyrazolo [1, 5-a] pyrimidin-3-yl] quinoline to preparation of autophagy inhibitor or tumor sensitizing drug

A technology of isopropoxy and autophagy inhibition, applied in the field of biomedicine, can solve the problem of few autophagy inhibitors

Active Publication Date: 2013-03-06
HARBIN MEDICAL UNIVERSITY
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Problems solved by technology

At present, there are few autophagy inhibitors that elucidate the exact mechanism, and new autophagy inhibitors need to be discovered to provide new research tools for autophagy research

Method used

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  • Application of 4-[6-(4-isopropoxypheny) pyrazolo [1, 5-a] pyrimidin-3-yl] quinoline to preparation of autophagy inhibitor or tumor sensitizing drug
  • Application of 4-[6-(4-isopropoxypheny) pyrazolo [1, 5-a] pyrimidin-3-yl] quinoline to preparation of autophagy inhibitor or tumor sensitizing drug
  • Application of 4-[6-(4-isopropoxypheny) pyrazolo [1, 5-a] pyrimidin-3-yl] quinoline to preparation of autophagy inhibitor or tumor sensitizing drug

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Embodiment 1

[0021] 1. Cells and experimental reagents:

[0022] MCF-7 cells (Cell Bank of Chinese Academy of Sciences), 4-[6-(4-isopropoxy)pyrazolo[1,5-a]pyrimidin-3-yl]quinoline, Rapamycin, AICAR were purchased from Sigma Aldrich Company; DMEM / high glucose medium and DMEM / low glucose medium were purchased from HYCLONE Company, trypsin was purchased from Invitrogen Company, and fetal bovine serum was purchased from Gibco Company.

[0023] 2. Solution preparation:

[0024] PBS buffer: 0.2g, Na2HPO4·12H 2 o 2 3.48g, KH 2 PO 4 0.02g, dissolved in 1000ml deionized water, aliquoted, and stored at 4°C for later use.

[0025] 0.25% trypsin digestion solution: trypsin TRYPSIN 0.25g, EDTA-2Na 0.02g and PBS buffer 100mL, and adjust the pH to 7.2.

[0026] 4-[6-(4-isopropoxy)pyrazolo[1,5-a]pyrimidin-3-yl]quinoline: Dissolve 25mg powder in 5ml DMSO, filter, store at 4°C, stock solution concentration: 1 mg / ml.

[0027] Rapamycin: Dissolve 1mg powder in 1ml DMSO, filter, store at -20°C, stock...

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Abstract

The invention discloses application of 4-[6-(4-isopropoxypheny) pyrazolo [1, 5-a] pyrimidin-3-yl] quinoline to preparation of autophagy inhibitors or tumor sensitizing drugs, belonging to the field of biomedicine. According to researches, the 4-[6-(4-isopropoxypheny) pyrazolo [1, 5-a] pyrimidin-3-yl] quinoline can inhibit autophagy induced by hunger, AICAR (5-Aminoimidazole-4-carboxamide 1-beta-D-ribofuranoside) and rapamycin by activating an Akt-mTOR signal pathway. According to further researches, the 4-[6-(4-isopropoxypheny) pyrazolo [1, 5-a] pyrimidin-3-yl] quinoline can enhance the breast cancer cell resisting effect of tamoxifen. Therefore, the application of 4-[6-(4-isopropoxypheny) pyrazolo [1, 5-a] pyrimidin-3-yl] quinoline disclosed by the invention has wide application prospect in preparation of autophagy inhibitors or tumor sensitizing drugs.

Description

technical field [0001] The present invention relates to a new application of 4-[6-(4-isopropoxy)pyrazolo[1,5-a]pyrimidin-3-yl]quinoline, in particular to 4-[6-(4- Use of isopropoxy)pyrazolo[1,5-a]pyrimidin-3-yl]quinoline in the preparation of autophagy inhibitors or tumor sensitization drugs. The invention belongs to the field of biomedicine. Background technique [0002] Autophagy is a process in which some damaged proteins or organelles in cells are wrapped by autophagic vesicles with a double-membrane structure, and then transferred to lysosomes for degradation and recycling. Autophagy is a very important biological phenomenon that participates in various processes such as the development and growth of organisms. The currently discovered autophagy inducers mainly include 1) Bredeldin A / Thapsigargin / Tunicamycin; 2) Carbamazepine, Lithium Chloride (lithium chloride), 3) Earle's balanced salt solution, 4) N-Acetyl-D-sphingosine, 5) Rapamycin , 6) Xestospongin B / C; autopha...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61K31/138A61P35/00
Inventor 董德利生悦孙博孙志浩杨宝峰
Owner HARBIN MEDICAL UNIVERSITY
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