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<131>I-labeled vascular endothelial growth factor receptor2 (VEGFR2)-resistant chimeric Fab and use thereof

A 131I-FA8H1, labeling technology, applied in the field of biomedicine, can solve the problems of disordered arrangement of blood vessels and difficult to obtain effects of anti-tumor drugs, so as to induce apoptosis of liver cancer cells, reduce immunity and inhibit tumor growth. Effect

Inactive Publication Date: 2013-10-02
NANJING MEDICAL UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The important reason is that the arrangement of blood vessels in the liver cancer tissue is disordered and irregular, coupled with the high pressure inside the tumor, it is difficult to achieve good results with traditional methods of anti-tumor drugs

Method used

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  • &lt;131&gt;I-labeled vascular endothelial growth factor receptor2 (VEGFR2)-resistant chimeric Fab and use thereof
  • &lt;131&gt;I-labeled vascular endothelial growth factor receptor2 (VEGFR2)-resistant chimeric Fab and use thereof
  • &lt;131&gt;I-labeled vascular endothelial growth factor receptor2 (VEGFR2)-resistant chimeric Fab and use thereof

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Embodiment 1

[0032] 1) FACS: Culture BEL-7402, QCY-7701, SMMC-7721, HepG2 and SK-HEP-1 to the logarithmic growth phase respectively; refer to the above method, detect the difference in the expression level of VEGFR2 in the natural conformation of different liver cancer cell lines by FACS, The concentration of FA8H1 was 10 μg / mL. The results were shown as: SMMC-7721 (67.21%), SK-HEP-1 (72.35%), HepG2 (80.45%), QCY-7701 (84.94%), BEL-7402 (93.73%), among which the expression of native conformation VEGFR2 was the highest It is the liver cancer cell line BEL-7402.

[0033] 2) Radioactive isotopes 131 I mark FA8H1 (conducted in a fume hood in a professional laboratory):

[0034] Chloramine-T oxidation method (Chloramine-T), the following is the proportion of each reagent: 100 μg FA8H1 plus 200 μL PB (0.2 M, pH 8.0); at the same time add 60 μL about 74 MBq Na 131 I (2.0 mCi) was mixed evenly, and then 100 μL of the oxidant chloramine-T (3 mg / mL) was added, and the reaction was shaken at room ...

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Abstract

The invention discloses a <131>I-labeled vascular endothelial growth factor receptor2 (VEGFR2)-resistant chimeric Fab and a use thereof. The <131>I-labeled VEGFR2-resistant chimeric Fab is prepared by a chloramines-T oxidation technology. The preparation method of the <131>I-labeled VEGFR2-resistant chimeric Fab comprises of labeling VEGFR2-resistant chimeric Fab by <131>I, carrying out separation purification of <131>I-FA8H1, and determining radiochemical purity and specific activity. The <131>I-labeled VEGFR2-resistant chimeric Fab is suitable for radionuclide image-based liver cancer diagnosis. The <131>I-FA8H1 is used for targeted treatment on liver cancer, can effectively inhibit cancer growth, has effects obviously superior to effects of single FA8H1 or <131>I, can promote large-area necrosis of cancer tissue, can induce liver cell apoptosis, and does not inhibit peripheral blood wbc for a long time thereby preventing the side effect of reducing immunity. Therefore, the <131>I-labeled VEGFR2-resistant chimeric Fab can be used for preparation of a drug for treating liver cancer.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and specifically relates to a 131 I-labeled anti-VEGFR2 chimeric Fab and its application. Background technique [0002] Primary liver cancer (hereinafter referred to as liver cancer) is one of the most common malignant tumors in the world. According to the World Health Organization, there are about 630,000 new cases and 600,000 deaths each year worldwide. Most of the diagnosed liver cancer patients are in Died within a year. my country is one of the areas with a high incidence of liver cancer in the world, and the occurrence of liver cancer accounts for about 55% of all cases in the world. Qidong City in Nantong, Jiangsu Province is a high incidence area of ​​liver cancer in my country. At present, the most effective treatment for liver cancer is early liver cancer surgery. By the time the patient finds symptoms, the liver cancer has entered the middle and late stages, often involving multi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/10A61P35/00
Inventor 冯振卿黄剑飞朱进咸华咸云唐小军唐奇
Owner NANJING MEDICAL UNIV