Medicament for treating tumor with csf1r as drug target and preparation method thereof
A technology of drugs and oils, which is applied in the field of drugs for treating tumors and its preparation, can solve the problems of high recurrence rate, inability to remove the cause of disease, uncertain cause of disease, etc., and achieve the effect of improving prognosis
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[0037] In order to solve the above technical problems, the present invention provides an application of CSF1R: as a therapeutic target of Langerhans cell tumor or tumor-associated macrophages, to prepare a medicament and a preparation method.
[0038] The present invention provides the application of CSF1R as a drug target in the treatment of Langerhans cell tumors or tumor-associated macrophages. The CSF1R is a transmembrane receptor of tyrosine kinase and CSF1 / Member of the PDGF receptor family.
[0039] The specific protein sequence of CSF1R in Rattus norvegicus is:
[0040]
[0041]
[0042] The specific protein sequence of CSF1R in humans is:
[0043]
[0044] The present invention provides a medicament for treating Langerhans cell tumor or tumor-associated macrophages with CSF1R as a drug target, that is, oral oil preparation of Ki20227 is used to antagonize CSF1R. Ki 20227 acts as an antagonist of CSF1R.
[0045] The molecular mass of Ki 20227 is 480.54, an...
example 1
[0051] Example 1: The present invention provides a new target for the treatment of Langerhans cell tumor - CSF1R. Specifically, mice were treated with CSF1R antagonist Ki 20227 oral oil and CSF1R inhibitory monoclonal antibody vehicle (eg figure 2 ), Langerhans cells (CD45+CD11b+epCAM+) were screened out by flow cytometry (such as image 3 ), the proportion of Langerhans cells was compared with that of the control group, and the proportion of Langerhans cells in the two groups of mice treated with Ki 20227 and CSF1R inhibitory monoclonal antibody were significantly reduced (such as Figure 4 A, 4B).
[0052] Further, the immunofluorescence technique was used to verify that the Langerhans cells in the mouse skin were significantly reduced after treatment with Ki 20227 and CSF1R inhibitory monoclonal antibody compared with those before treatment (such as Figure 5 ).
[0053] The two medicaments for targeting and inhibiting Langerhans cell tumors provided by the present inve...
Embodiment approach
[0055] Implementation method: Dissolve 0.5g Ki 20227 in 5ml 50% DMSO, add to 30ml monooleate after dissolving, heat to 40°C, mix well, add 65ml oleic acid, mix well, and then make 5mg / ml Ki 20227 oral oil formulation.
[0056] 2. A method for preparing a CSF1R inhibitory monoclonal antibody solvent.
[0057] Implementation method: Add 1 mg of anti-mouse CSF1R (CD115) with the clone number AFS98 into 2 ml of PBS containing 0.1% BSA at 4°C, mix thoroughly to obtain a 500 μg / ml CSF1R inhibitory monoclonal antibody solvent, and store at 4°C.
[0058] CSF1R antagonist Ki 20227 oral oil and CSF1R inhibitory monoclonal antibody solution can reduce Langerhans cells in Langerhans cell tumors.
[0059] 1. Flow cytometry analysis of the effects of Ki 20227 oral oil preparation and CSF1R inhibitory monoclonal antibody solution on mouse Langerhans cells.
[0060] Implementation method: Treat mice with CSF1R antagonist Ki 20227 oral oil and CSF1R inhibitory monoclonal antibody solution re...
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