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Somatostatin analogue for detecting cancers as well as preparation method and application thereof

A technology of somatostatin and analogues, which is applied in the field of biomedicine, can solve the problem of no suggested cancer markers, etc., and achieve intuitive and accurate labeling results, accurate results, and high stability

Inactive Publication Date: 2018-08-24
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, while the value of this tumor marker as a diagnostic or prognostic factor has been studied, it has so far been of limited use and there are still no cancer markers proposed for official use

Method used

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  • Somatostatin analogue for detecting cancers as well as preparation method and application thereof
  • Somatostatin analogue for detecting cancers as well as preparation method and application thereof
  • Somatostatin analogue for detecting cancers as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0044] The somatostatin analog of the above-mentioned structure of the present invention is preferably synthesized by a 9-fluorenylmethoxycarbonyl solid-phase synthesis method, and the solid-phase synthesis method comprises the following steps: making the solid-phase synthesis resin Fmoc-Thr(tBu)-Ol-2-Cl -After Trtresin swells, wash and remove Fmoc to obtain de-Fmoc resin; Fmoc-Cys(Trt)-OH, Fmoc-Thr(tbu)-OH, Fmoc-Lys(Boc)-OH, Fmoc-D-Trp(Boc) )-OH, Fmoc-Tyr(tbu)-OH, Fmoc-Cys(Trt)-OH, Fmoc-D-Phe-OH and Boc-HYNIC are coupled to the de-Fmoc resin to form a peptide bond, and the reaction in the resin is collected The obtained polypeptide is oxidized to obtain the somatostatin analog.

[0045] First, the solid-phase synthetic resin Fmoc-Thr(tBu)-Ol-2-Cl-Trtresin is swollen, washed and removed from Fmoc to obtain the de-Fmoc resin. Said swelling and washing preferably use dimethylformamide. The present invention preferably reacts with resin with the volume concentration of 25% pipe...

Embodiment 1

[0057] Synthesis and Purification of Polypeptide HYNIC-TOC

[0058] 1. Main reagents:

[0059] Fmoc-Thr(tBu)-Ol-2-Cl-Trt 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 ), ethanedithiol (EDT), acetonitrile (ACN), pure water (H 2 O), phosphate buffered saline (PBS), Kaiser reagent.

[0060] Second, the main equipment:

[0061] 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-2000), freeze-drying machine (Boyikang FD-1).

[0062] Three, the synthesis process (see figure 1 ):...

Embodiment 2

[0097] The HYNIC-TOC prepared in Example 1 was sent to Midu (Nanjing) Biotechnology Co., Ltd. 99m Tc mark, get 99m Tc-HYNIC-TOC. right 99m The stability of Tc-HYNIC-TOC was determined

[0098] 1. Quality control and solvent stability testing

[0099] Using the Radio-iTLC method for 99m The radiochemical purity of Tc-HYNIC-TOC was tested, the support was silica gel impregnated glass fiber strips, and the developing agents were 50% acetonitrile and 0.5M citric acid / sodium citrate buffer (pH=5).

[0100] Utilize Radio-iTLC pair 99m Tc-HYNIC-TOC conducts quality control and in vitro solvent stability testing, and the results show that:

[0101] 99m The quality control of Tc-HYNIC-TOC (L17091801 and L17091901) was qualified, and the radiochemical purity (RCP) was 100%, meeting the test requirements.

[0102] 2. In vitro stability of the test object

[0103] 99m Tc-HYNIC-TOC was stored in 0.2M PB buffer (pH=6) at room temperature, its radiochemical purity was detected by R...

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PUM

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Abstract

The invention provides a somatostatin analogue. A polypeptide sequence of the somatostatin analogue is as follows: HYNIC-D-Phe-cyclo[Cys-Tyr-D-Trp-Lys-Thr-Cys]-L-threoninol. The somatostatin analogueor an analogue thereof is synthesized by adopting a 9-fluorenylmethoxycarbonyl solid-phase synthesis (FMOC-SPPS) method. The 99mTc-lableled 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, in particular to a somatostatin analog for cancer detection, 99m TC-labeled somatostatin analogue and its preparation method and application. Background technique [0002] Cancer is one of the malignant tumors with the fastest increasing morbidity and mortality, and the greatest threat to the health and life of the population. Cancer usually has some symptoms due to the growth of cancer cells and invasion of surrounding tissues. However, there are also about 10-15% of patients without any symptoms, which can only be diagnosed through regular physical examinations. In addition, most cancers have developed to stage III (3) or above when they are discovered, and are generally difficult to cure. Therefore, early diagnosis of cancer to reduce mortality due to cancer is an urgent issue. [0003] In order to diagnose cancer, a variety of methods are generally used comprehensively. So far, most of them have...

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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