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A 99mtc-labeled somatostatin analog for lung cancer diagnosis and its preparation method

A technology for 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 intuitive and accurate labeling results, high yield, and good separation effect.

Active Publication Date: 2021-06-01
上海欣科医药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, although the value of this tumor marker as a diagnostic or prognostic factor has been investigated, so far it has been of limited use, and there is still no proposed official use of lung cancer markers.

Method used

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  • A 99mtc-labeled somatostatin analog for lung cancer diagnosis and its preparation method
  • A 99mtc-labeled somatostatin analog for lung cancer diagnosis and its preparation method
  • A 99mtc-labeled somatostatin analog for lung cancer diagnosis and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

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 object of the present invention is to provide a kind of somatostatin analog, described somatostatin analog is the aminoacid sequence Hynic-D-Phe-cyclo[Cys-Tyr-D-Trp-Lys-Thr-Cys]-Thr-NH 2 ; Somatostatin analog molecular formula is C 55 h 70 N 14 o 12 S 2 . The present invention also provides a preparation method for the above-mentioned somatostatin analogue or its analogue, which is synthesized by 9-fluorenylmethoxycarbonyl solid-phase synthesis (FMOC-SPPS) method or Fmoc-tBu solid-phase synthesis method. described in the present invention 99m Tc-labeled somatostatin analogs have a high labeling rate and high stability, and can be directly labeled. Cell experiments and rat experiments have proved that the labeling of the present invention can intuitively reflect the tumor location of each organ, and the results are 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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Patent Type & Authority Patents(China)
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