Application of compound PS-341 in preparation of medicine for treating acute pulp leucocythemia
A technology for PS-341 and acute myeloid leukemia, which is applied in the application field of compound PS-341 in the preparation of drugs for the treatment of acute myeloid leukemia, and can solve the problem of median survival time of less than 2 years, survival rate of less than 40%, treatment failure, etc. problems, to achieve the effects of easy changes in blood drug concentration, significant curative effect, and convenient medication
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Examples
Embodiment 1
[0023] U937 cells transfected with AML1-ETO fusion gene (U937-A / E cells) were treated with different concentrations of PS-341, and after 24 hours of treatment, the cells were collected and lysed with 1× cell lysate to extract protein, and then treated with anti-ETO antibody ( (purchased from Santa Cruz, USA) for Western blot immunoblotting experiments. It was found that PS-341 could regulate the expression of AML1-ETO fusion protein, partially degrade the AML1-ETO protein and produce degradation bands, see figure 1 , where the left is the control, and the right is the change of AML1-ETO fusion protein after 24 hours of treatment with PS-341 at a concentration of 10 nM.
Embodiment 2
[0025] With different concentrations of compound PS-341 (1×10 -10 ~1×10 -5 M) Treat Kasumi-1 cells, add 2-(2-methoxy-4-nitrophenyl)-3-(4-nitrophenyl)-5-(2,4-disulfonic acid) after 44 hours Acid phenyl)-2H-tetrazolium monosodium salt (WST-8) CCK-8 detection reagent, and then incubated for 4 hours, then measured its absorbance at 450nm (OD 450 ). It was found that PS-341 treatment could significantly reduce the OD of Kasumi-1 cells 450 , PS-341 can significantly inhibit the proliferation of Kasumi-1 cells, and the inhibition rate is positively correlated with the drug concentration (see figure 2 ). According to the growth inhibitory effect of PS-341 on Kasumi-1 cells, calculate the half maximal inhibitory concentration (IC) of PS-341 on Kasumi-1 cells 50 ) is 5.2×10 -9 M.
Embodiment 3
[0027]Kasumi-1 cells were treated with different concentrations of PS-341 (0.1nM~5nM)PS-341, and the number of viable cells was counted by placepan blue exclusion method at 12, 24, and 48 hours after treatment, and the number of Kasumi-1 cells was plotted. According to the growth curve, it was found that PS-341 could significantly inhibit the growth of Kasumi-1 cells, and this effect was time-dose dependent. When the concentration of PS-341 was 1-5nM, the number of living cells of Kasumi-1 treated with PS-341 was significantly reduced, as shown in image 3 shown.
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Abstract
Description
Claims
Application Information
- IPC
- A61K38/55; A61P35/02; A61K31/704; A61K38/19
- Inventors
- 周光飚; 谢军