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Application of pan-HDAC inhibitor to preparation of drug used for treating uveal melanoma

A technology for melanoma and grape tumor, applied in drug combination, antitumor drugs, pharmaceutical formulations, etc., can solve the problems of unclear efficacy and mechanism of uveal melanoma, and achieve improved treatment effectiveness, improved quality of life, prolonged Effects on patient lifespan

Active Publication Date: 2017-06-30
SHANGHAI NINTH PEOPLES HOSPITAL SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

PCI-24781 (Abexinostat) is a new type of pan-HDAC inhibitor. So far, there is no report on the application of PCI-24781 (Abexinostat) in uveal melanoma. clear

Method used

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  • Application of pan-HDAC inhibitor to preparation of drug used for treating uveal melanoma
  • Application of pan-HDAC inhibitor to preparation of drug used for treating uveal melanoma
  • Application of pan-HDAC inhibitor to preparation of drug used for treating uveal melanoma

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] IC50 determination experiment

[0017] Experimental materials: PCI-24781 (Abexinostat) was purchased from Selleck (China), and the cell-title glo kit was purchased from Promega (USA)

[0018] Experimental procedure: OCM1 and OM431 cells were seeded in a 384-well plate, 2500 cells per well, 50ul culture medium, 10 concentration gradients were added to PCI-24781 (Abexinostat), 37 ° C, 5% CO2 After 72 hours of culture, add cell-title The glo reagent was incubated at room temperature for 10 minutes, tested on the computer, and calculated IC50 according to the measured experimental results, that is, the median lethal dose. See the experimental results figure 1 shown.

Embodiment 2

[0020] Plate cloning experiments

[0021] Experimental procedure: OCM1 and OM431 cells were seeded in a 6-well plate, 1000 cells per well, 2ml of culture medium, 5 concentration gradients were added to PCI-24781 (Abexinostat), 37 ° C, 5% CO2 After 7 days of culture, crystal violet staining, See the experimental results figure 2 shown. It can be seen that PCI-24781 (Abexinostat) inhibits the proliferation of uveal melanoma cells in a concentration-dependent manner.

Embodiment 3

[0023] Cell Proliferation Assay (CCK8)

[0024] Experimental materials: CCK8 was purchased from Japan Tongren Chemical Co., Ltd.

[0025] OCM1 and OM431 cells were seeded in 96-well plates, 5000 cells per well, 100ul culture medium, 10umol PCI-24781 (Abexinostat), 37°C, 5% CO2 culture, 10ul CCK8 was added at 0h, 24h, 48h, and 72h respectively, and continued Incubate at 37°C for 4 hours, and measure the absorbance value on the computer. The results are as follows: image 3 shown. It can be seen that PCI-24781 (Abexinostat) can significantly inhibit the proliferation of uveal melanoma cells.

[0026] The present invention finds for the first time that PCI-24781 (Abexinostat) can significantly inhibit the growth of uveal melanoma cells, and the effect of the drug increases as the concentration increases. The invention aims to provide new therapeutic drugs for the clinical treatment of uveal melanoma, improve the effectiveness of treatment, prolong the life of patients and impr...

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Abstract

The invention provides application of a pan-HDAC inhibitor to preparation of a drug used for treating uveal melanoma. The pan-HDAC inhibitor is PCI-24781 and has a molecular formula of C21H23N3O5; and the molecular structural formula of the pan-HDAC inhibitor is as shown in a formula I which is described in the specification. It is found for the first time that the PCI-24781 (abexinostat) can substantially inhibit cell growth of uveal melanoma and drug effect is improved with concentration increase. The objective of the invention is to provide a novel clinical treatment drug for uveal melanoma, and the novel clinical treatment drug can improve treatment effectiveness, prolong the life of a patient and enhance quality of life. A novel field is opened up in the invention.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the application of pan-HDAC inhibitors in the preparation of medicines for treating grape tumor melanoma. Background technique [0002] Uveal melanoma (Uveal melanoma, UM) is a special type of melanoma originating from the uveal layer of the eye. UM is the most common primary intraocular malignancy in adults, the majority of which are choroidal melanomas. UM usually occurs unilaterally and unifocally, but rare cases of bilateral or multifocal tumors within the same eye occur. UM can not only cause vision loss, but also seriously threaten the life of patients. UM mainly metastasizes through blood, and half of the patients can develop distant metastases, mainly to the liver. Once the diagnosis is established, it is usually fatal within 1 year, because there is currently no effective clinical treatment. Even if the affected eye is enucleated before definite metastasis occurs, the 5-year ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/343A61P35/00
CPCA61K31/343
Inventor 张赫范先群王茜文旭洋柴佩韦葛盛芳贾仁兵
Owner SHANGHAI NINTH PEOPLES HOSPITAL SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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