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Application of apatinib to preparing BRAF V600E protein kinase inhibitors

A protein kinase inhibitor, apatinib technology, which is used in the application field of apatinib to prepare a BRAFV600E mutant tumor drug, and can solve problems such as no literature reports on the inhibitory effect of BRAFV600E protein kinase.

Inactive Publication Date: 2017-08-18
SECOND AFFILIATED HOSPITAL SECOND MILITARY MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] At present, there are no reports on the inhibitory effect of apatinib on BRAF V600E protein kinase, and the therapeutic effect of apatinib on patients with BRAF V600E mutant tumors

Method used

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  • Application of apatinib to preparing BRAF V600E protein kinase inhibitors
  • Application of apatinib to preparing BRAF V600E protein kinase inhibitors
  • Application of apatinib to preparing BRAF V600E protein kinase inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1. In vitro inhibitory screening of apatinib on various kinases

[0029] Apatinib was used to prepare a 100nM solution with DMSO, and 138 protein kinase libraries were screened based on Life's LanthaScreenbinding and ZLYTE platforms. The results showed that, in addition to the known targets VEGFR2 and KIT, apatinib can bind to BRAF V600E protein kinase, and has a good inhibitory activity on it, with an inhibition rate of 51%.

Embodiment 2

[0030] Example 2. Inhibitory Effect of Apatinib on the Growth of Human Melanoma and Colorectal Cancer Cell Lines in Vitro

[0031] Human melanoma cells (A375, SK-MEL-28) and colorectal cancer cells (Colo205, HT29) in the logarithmic growth phase were taken, and the cell suspension was prepared by trypsinization method, and the cell pellet was collected by centrifugation. RPMI1640 complete medium (the final concentrations of apatinib were 0, 50, 100, 200, 400, 800 nM) to adjust the cell density to 1 × 10 5 cells / mL, inoculate cells into 96-well cell culture plate, add 100 μL cell suspension to each well, shake the culture plate to make it evenly distributed, 37 and 5% CO 2 The cells were cultured under these conditions, and the cell viability was detected by CCK-8 method 48 hours after inoculation. Before detection, add 10 μL of CCK-8 solution to each well of cells, shake gently to make it evenly distributed, and store at 37 and 5% CO 2 Continue culturing for 4 hours, detect ...

Embodiment 3

[0033] Example 3. Inhibitory Effect of Apatinib on MAPK Signaling Pathway

[0034] Human melanoma A375 cells in the logarithmic growth phase were taken, and the cell suspension was prepared by trypsinization method, and the cell pellet was collected by centrifugation, and the cell density was adjusted to 1×10 5 cells / mL, inoculate cells into 6-well cell culture plate, add 2mL cell suspension to each well, gently shake the culture plate to make the distribution even, 37 and 5% CO 2 Cultivate under conditions, and remove the medium 3 hours after inoculation, add 1mL dPBS to the culture plate to wash the cells twice, remove the dPBS, add 0.5mL cell lysate to each well, extract the total cell protein according to the kit instructions, and quantify it by BCA method Total cell protein concentration. Quantified total cell protein, 10 μL per group for vertical electrophoresis, SDS-polyacrylamide gel separation gel concentration is 10%, after 90 minutes of electrophoresis at 110V vol...

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PUM

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Abstract

The invention relates to the technical field of medicines, in particular to application of apatinib to preparing BRAF V600E protein kinase inhibitors and application of the apatinib to preparing medicines for treating BRAF V600E mutation tumor. Melanoma, thyroid papillary carcinoma, borderline ovarian tumor, colorectal cancer, non-small cell lung cancer and hairy cell leukemia can be treated by the medicines. The application has the advantages that novel targets and indication can be provided for the apatinib; novel thinking can be provided for treating tumor such as BRAF V600E mutation melanoma, colorectal cancer and non-small cell lung cancer.

Description

technical field [0001] The invention relates to the technical field of medicine, specifically, the application of apatinib in the preparation of BRAF V600E protein kinase inhibitors, and the application of apatinib in the preparation of drugs for treating BRAF V600E mutation tumors. Background technique [0002] Apatinib Mesylate Tablets, C 24 h 23 N 5 O·CH 4 o 3 S, hereinafter referred to as apatinib) is a Class 1.1 new drug independently developed in my country. It was approved for marketing in 2014 and is used for the third-line or later treatment of advanced gastric adenocarcinoma or gastroesophageal junction adenocarcinoma. In addition, clinical trials of apatinib for lung cancer, breast cancer and liver cancer have shown that it has a good effect on a variety of solid tumors (see literature: ZHANG H. Apatinib for molecular targeted therapy in tumor[J].Drug design ,development and therapy,2015,9:6075-6081.), suggesting that apatinib has a good application prospect....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/444A61P35/00G01N33/574
CPCA61K31/444G01N33/57423G01N33/57446G01N33/57484
Inventor 陈万生位华龚晓斌王军刘诗怡陶霞张凤高守红夏天一
Owner SECOND AFFILIATED HOSPITAL SECOND MILITARY MEDICAL UNIV
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