Use of XRK3F2 in preparation of medicine for treating leukemia

A leukemia and leukemia stem cell technology, applied in the field of XRK3F2 in the preparation of drugs for the treatment of leukemia, can solve the problems of lack of specificity, different effects of different cell types, and low target specificity, and achieve a good inhibitory effect

Inactive Publication Date: 2020-12-25
INST OF HEMATOLOGY & BLOOD DISEASES HOSPITAL CHINESE ACADEMY OF MEDICAL SCI & PEKING UNION MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, many drugs that activate or inhibit autophagy lack specificity, inc

Method used

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  • Use of XRK3F2 in preparation of medicine for treating leukemia
  • Use of XRK3F2 in preparation of medicine for treating leukemia
  • Use of XRK3F2 in preparation of medicine for treating leukemia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029]A small molecule inhibitor XRK3F2 targeting p62, its structure is:

[0030]

Embodiment 2

[0032]XRK3F2 cell line level analysis includes the following steps:

[0033]The CCK8 method was used to verify the killing activity of XRK3F2 against leukemia cell lines and drug-resistant leukemia cells, and passed IC50Analysis shows that XRK3F2 has obvious killing effect on leukemia cell lines and drug-resistant leukemia.

[0034]1) CCK8 method to detect the killing of XRK3F2 on leukemia cell lines:

[0035](1) Resuscitate cryopreserved tumor cell lines (HL60, HL60 / ADR, K562, K562 / A02) from liquid nitrogen. The frozen cells were removed from liquid nitrogen and placed in a 37°C water bath. After thawing, they were centrifuged at 1000 rpm for 8 minutes, and resuspended in fresh 1640 medium. Put it into a 37°C cell incubator for culture.

[0036](2) When the cells are in the logarithmic phase, collect a certain amount of cells and adjust the cell concentration to 2.5×104 / ml (ie 5×103cell / well / 90μL). Add 90μL per well to a 96-well plate, and supplement the edge wells with sterile PBS.

[0037](3) D...

Embodiment 3

[0050]The analysis of the killing effect of XRK3F2 on leukemia stem cells derived from MLL-AF9 AML leukemia mice includes the following steps:

[0051]The Annexin V-7AAD apoptosis detection method was used to verify the killing activity of XRK3F2 on mouse primary leukemia cells. Statistical analysis of the ratio of viable cells showed that XRK3F2 had a significant killing effect on mouse primary leukemia cells, and its IC50With a value of 8μM, XRK3F2 has a significant killing effect on mouse primary leukemia stem cells, and its IC50The value is 6 μM.

[0052]1) The Annexin V-7AAD apoptosis detection method detects the killing of mouse primary leukemia cells by XRK3F2:

[0053](1) Mouse primary leukemia cells were isolated from femur, tibia and iliac bones of MLL-AF9 AML leukemia mice, placed in fresh IMDM medium, and placed in a 37°C cell incubator with 5% CO2To cultivate.

[0054](2) When the cells grow to a uniform size, collect a certain amount of cells and adjust the cell concentration to 1...

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Abstract

The invention relates to the field of medicines, in particular to a use of XRK3F2 in the preparation of a medicine for treating leukemia. The p62 small-molecule inhibitor XRK3F2 disclosed by the invention has good inhibition effects on MLL-AF9 AML mouse leukemia stem progenitor cells and human leukemia stem progenitor cells, and a new method can be provided for future clinical treatment.

Description

Technical field[0001]The invention relates to the field of medicine, in particular to the use of XRK3F2 in the preparation of medicines for treating leukemia.Background technique[0002]Leukemia is a common malignant tumor of the blood system. Acute Myeloid Leukemia (AML) is the most common type of malignant clonal hematopoietic system disease originating from hematopoietic stem and progenitor cells among all leukemias. Inferior, tumor heterogeneity is high, and the problem of drug resistance relapse easily occurs in the elderly and children. It is currently believed that leukemia stem cells (LSCs), as a group of tumor cells with the characteristics of stem cells in AML, are not only the origin of the malignant clone of leukemia, but also the root cause of the drug resistance and recurrence of leukemia. So far, the classic AML treatment regimen is still based on the remission induction regimen of anthracyclines combined with cytarabine ("7+3" chemotherapy regimen) and allogeneic hemat...

Claims

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Application Information

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IPC IPC(8): A61K31/137A61P35/02
CPCA61K31/137A61P35/02
Inventor 高瀛岱李迎辉李亚芳杨铭尹晶晶王超群张文姗何媚徐惠
Owner INST OF HEMATOLOGY & BLOOD DISEASES HOSPITAL CHINESE ACADEMY OF MEDICAL SCI & PEKING UNION MEDICAL COLLEGE
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