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Application of erlotinib in preparation of FLT3 inhibitor-type medicine

An inhibitor and drug technology, which can be used in drug combinations, antitumor drugs, pharmaceutical formulations, etc., can solve the problem of no erlotinib inhibiting FLT3 enzyme activity, and achieve good clinical application prospects, good effects, and strong inhibitory effects. Effect

Inactive Publication Date: 2019-07-30
CHENGDU UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, there is no report that erlotinib inhibits FLT3 enzyme activity or is used for the treatment of leukemia

Method used

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  • Application of erlotinib in preparation of FLT3 inhibitor-type medicine
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  • Application of erlotinib in preparation of FLT3 inhibitor-type medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1, the enzymatic level inhibitory activity of erlotinib to FLT3 kinase

[0028] 1. Experimental materials

[0029] Liquid container, 384 plate, multi-label microplate detector (Perkin Elmer), KinEASETM and FMS-like tyrosine kinase 3 (FLT3) were purchased from Beijing Yiqiao Shenzhou.

[0030] 2. Experimental method

[0031] The experiment was operated according to the optimization program provided in the HTRF kit, and the experimental data were fitted by Graphpad software.

[0032] 3. Experimental results

[0033] From figure 1 It can be seen that in the enzyme level activity test, erlotinib exhibited a significant inhibitory effect on FLT3, indicating that the drug can produce corresponding pharmacodynamic effects by inhibiting the activity of FLT3.

Embodiment 2

[0034] Example 2, Erlotinib inhibits FLT3 activity in MV4-11 cells

[0035] 1 Experimental materials

[0036] 1.1 Main reagents

[0037] IMDM medium, fetal calf serum, and trypsin were purchased from Gibco (Life technologies corporation).

[0038] FLT3 and p-FLT3 antibodies were purchased from cell signaling technology company.

[0039] 1.2 Cell lines

[0040] The MV4-11 cell line was purchased from ATCC, USA.

[0041] 2 Experimental methods

[0042] After the MV4-11 cells were treated with gradient concentrations of erlotinib (20, 10, 5, 2.5 μM) for 20 h, the cells were collected by centrifugation and lysed with RIPA to extract the total intracellular protein. Then, the protein was separated by SDS-PAGE electrophoresis separation and PVDF membrane transfer and transferred to PVDF membrane. Subsequently, they were blocked by FBS, immunocombined with FLT3 or p-FLT3 antibody, and incubated with secondary antibody. Finally, the effects of different concentrations of erloti...

Embodiment 3

[0045] Embodiment 3, in vitro anti-tumor cell proliferation experiment of erlotinib

[0046] 1 Experimental materials

[0047] 1.1 Main reagents

[0048] RPMI-1640 and IMDM medium, fetal calf serum, and trypsin were purchased from Gibco (Life technologies corporation).

[0049] Dimethylsulfoxide (DMSO) and tetramethylazolium salt (MTT) were purchased from Sigma (USA).

[0050] Erlotinib was purchased from Nanjing Kangmanlin Technology Co., Ltd., and was prepared into a 20 mg / ml storage solution with 100% DMSO during in vitro experiments. It was stored in a -20°C refrigerator in the dark for future use, and was diluted to the required concentration with complete culture medium before use.

[0051] 1.2 Cell lines and culture

[0052] MV4-11 cell line, MOLM-13 cell line, and IL3-dependent proto-B lymphocyte Ba / F3 were purchased from ATCC in the United States, and Ba / F3-FLT3-ITD cells expressing FLT3-ITD protein were donated by Professor Yang Shengyong of Sichuan University . ...

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Abstract

The invention discloses application of erlotinib in preparation of an FLT3 inhibitor-type medicine and further discloses application of erlotinib in preparation of a medicine for treating leukemia. The erlotinib can inhibit the enzyme activity of FLT3, has an extremely-high inhibition function on FLT3-ITD mutant-type leukemia cells, has a good function of inhibiting leukemia in vivo, can have an inhibition function under the condition of a low side effect and is good in clinical application prospect.

Description

technical field [0001] The invention relates to the application of erlotinib in the preparation of FLT3 inhibitor drugs. Background technique [0002] Leukemia is a malignant clonal disease of hematopoietic stem cells. Clonal leukemia cells proliferate and accumulate in bone marrow and other hematopoietic tissues due to mechanisms such as uncontrolled proliferation, differentiation disorder, and apoptosis inhibition, and infiltrate other non-hematopoietic tissues and organs, while inhibiting normal hematopoietic function. Clinically, leukemia is often divided into lymphocytic leukemia, myeloid leukemia, mixed cell leukemia and so on. [0003] Acute myeloid leukemia (AML) is a malignant disease of myeloid hematopoietic stem / progenitor cells. It is mainly characterized by abnormal proliferation of primitive and immature myeloid cells in bone marrow and peripheral blood. The clinical manifestations are anemia, hemorrhage, infection and fever, visceral infiltration, and metabo...

Claims

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Application Information

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IPC IPC(8): A61K31/517A61P35/02A61P27/02A61P9/00
CPCA61K31/517
Inventor 曹治兴李玉芝彭成
Owner CHENGDU UNIV OF TRADITIONAL CHINESE MEDICINE
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