99mTC labeled somatostatin analogue for diagnosing lung cancer and preparation method thereof

A technology of somatostatin and analogs, applied in the field of biomedicine, can solve the problem of not recommending lung cancer labeling, etc., and achieve the effects of solving the confusion between labeled products and impurities, accurate results, and improved purity

Active Publication Date: 2018-08-24
上海欣科医药有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, although the value of this tumor marker as a diagnostic or prognostic factor has been investigat

Method used

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  • 99mTC labeled somatostatin analogue for diagnosing lung cancer and preparation method thereof
  • 99mTC labeled somatostatin analogue for diagnosing lung cancer and preparation method thereof
  • 99mTC labeled somatostatin analogue for diagnosing lung cancer and preparation method thereof

Examples

Experimental program
Comparison scheme
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Embodiment 1

[0029] Example 1 Polypeptide Synthesis and Purification and Labeling

[0030] 1. Main reagents and synthesis steps

[0031] (1) Main reagents:

[0032] Fmoc-Thr(tBu)-Rink-amide AM resin(0.3-0.6mmol / g), Fmoc-Cys(Trt)-OH, Fmoc-Thr(tbu)-OH, Fmoc-Lys(Boc)-OH, Fmoc- D-Trp(Boc)-OH, Fmoc-Tyr(tbu)-OH, Fmoc-D-Phe-OH, Boc-Hynic, HBTU, HOBt, Diisopropylethylamine (DIEA), Piperidine (PIP), Dimethylformamide (DMF), dichloromethane (DCM), methanol (MeOH), anhydrous methyl tert-butyl ether (MTBE), trifluoroacetic acid (TFA), triisopropylsilane (TIPS), ethyl Dithiol (EDT), acetonitrile (ACN), pure water (H2O), phosphate buffered saline (PBS), Kaiser reagent.

[0033] (2). HYNIC-Fpa(3)-TATE synthesis method route:

[0034] Main equipment:

[0035] Refrigerated centrifuge (Shanghai Luxiang TDZ5-WS), preparative high performance liquid chromatography (Chuangxin Tongheng LC6000), analytical high performance liquid chromatography (Thermo Fisher Ultimate 3000), mass spectrometer (Waters ZQ-200...

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Abstract

The invention aims at providing a somatostatin analogue. An amino acid sequence of the somatostatin analogue is as follows: Hynic-D-Phe-cyclo[Cys-Tyr-D-Trp-Lys-Thr-Cys]-Thr-NH2; a molecular formula ofthe somatostatin analogue is C55H70N14O12S2. The invention further provides a preparation method of the somatostatin analogue or an analogue thereof; the somatostatin analogue or the analogue thereofis synthesized by adopting a 9-fluorenylmethoxycarbonyl solid-phase synthesis (FMOC-SPPS) method or an Fmoc-tBu solid-phase synthesis method. The 99mTc-labeled somatostatin analogue provided by the invention has the advantages of relatively high labeling rate of a product, high stability and capability of directly labeling; a cell experiment and a mouse experiment prove that a label can be used for directly reflecting a tumor position of each organ and the result is accurate.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a 99mTC-labeled somatostatin analog for lung cancer diagnosis and a preparation method thereof. Background technique [0002] Lung cancer is one of the malignant tumors with the fastest growing morbidity and mortality, and the greatest threat to the health and life of the population. In the past 50 years, many countries have reported that the morbidity and mortality of lung cancer have increased significantly. The morbidity and mortality of lung cancer in men account for the first of all malignant tumors, and the incidence and mortality of lung cancer account for the second in women. The cause of lung cancer is still not fully understood. But along with reasons such as the increase of smoking population and air pollution, lung cancer is also a kind of tumor disease that increases sharply in our country. According to a recent survey by the Bureau of Statistics, its frequen...

Claims

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Application Information

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IPC IPC(8): C07K14/475C07K1/20C07K1/04A61K51/08A61K103/10
CPCA61K51/08C07K14/475
Inventor 徐鹏程吴松年夏伟张莉君
Owner 上海欣科医药有限公司
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