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Preparation method of targeting tumor vasculature Anxa1 marked precursor NOTA-IF7

A technology of NOTA-IF7 and tumor blood vessels, which is applied in the field of organic chemistry and medicine, can solve the problems of inability to capture mononuclear macrophage system and poor tumor penetration ability, and achieve high yield, simple preparation method and process reaction conditions mild effect

Inactive Publication Date: 2014-07-23
蒋孟军 +4
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, most targeted drugs used for diagnosis and treatment are monoclonal fragments, which have poor tumor penetration ability and cannot be specifically captured by the monocyte-macrophage system

Method used

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  • Preparation method of targeting tumor vasculature Anxa1 marked precursor NOTA-IF7
  • Preparation method of targeting tumor vasculature Anxa1 marked precursor NOTA-IF7
  • Preparation method of targeting tumor vasculature Anxa1 marked precursor NOTA-IF7

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1 Preparation of NOTA-IF 7:

[0022] (1) Dissolution: Weigh 8 mg of p-SCN-Bn-NOTA and dissolve in 50 μL DMSO to obtain solution a; weigh 20 mg IF 7 and dissolve in 300 μL dimethylformamide (DMF) to obtain solution b.

[0023] (2) Preparation of NOTA-IF 7: Add solution a and solution b prepared in step (1) into a glass bottle according to the mass ratio of NOTA:IF 7 1-2:1, and then add 50 μL of diisopropylethylamine (DIEA), react at 40°C for 2h, cool to room temperature, add 30μL acetic acid to the reaction solution to terminate the reaction.

Embodiment 2

[0024] The separation and purification method of embodiment 2 NOTA-IF 7:

[0025] (1) Preparative HPLC purification

[0026] NOTA-IF 7 was purified by preparative HPLC, Waters XBridge C-18 column 150 mm × 19 mm, 5 μm, mobile phase A was pure water containing 0.1% TFA, B was acetonitrile containing 0.1% TFA, flow rate was 20 mL / min, the injection volume is 1 mL, and the detection wavelength is 254nm.

[0027] (2) Gradient elution, the mobile phase composition was increased from 95% A and 5% B in 5 minutes to 35% A and 65% B in 24 minutes, and the fraction collected for about 15.3 minutes was NOTA-IF 7.

[0028] The HPLC separation and purification diagram of NOTA-IF 7 is as follows figure 1 shown. Mass spectrometry diagram as figure 2 shown.

Embodiment 3

[0030] Purity identification: the mass spectrometer is AB 4800 MALDI-TOF / TOF, the detection mode is reflection mode, the laser intensity is 4000, and the voltage is 0.95KV. The NOTA-IF 7 sample purified by HPLC was dissolved in 1 mL of 20% acetonitrile, and 0.1 μL of the target was taken. The measured molecular weight was 1425.6, which was consistent with the theoretical molecular weight, and it was confirmed to be a single NOTA-IF 7.

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Abstract

The invention relates to a preparation method of targeting tumor vasculature Anxa1 marked precursor NOTA-IF7, which belongs to the fields of organic chemistry and medicines. According to the invention, a double-function chelating agent 1,4,7-triazacyclononane-1,4,7- triaceticacid (1,4,7-triazacyclononane-1,4,7- triaceticacid, p-SCN-Bn-NOTA, NOTA for short) is coupled with specifically combined tumor vasculature 7 peptide amino acid (isoleucine-phenylalanine-leucine-leucine-tryptophan-glutamine-arginine, IF7), and a HPLC one-step method is used for purifying to obtain NOTA-IF7. THE preparation method of NOTA-IF7 is simple, the reaction condition of the technology is mild, the yield is high, the product can be used for isotope mark of fluorine-18, copper-64 and gallium-68, and is conveniently prepared to a positron photographic developer for tumor.

Description

technical field [0001] The invention discloses a method for preparing the Anxa1-targeted tumor vascular marker precursor NOTA-IF 7, which can be used in the development of tumor imaging agents, plays an important role in the development of tumor drugs and early diagnosis of tumors, and other biological application fields, and belongs to organic chemistry and pharmaceutical field. Background technique [0002] Cancer is a disease that seriously threatens human health. Early diagnosis and treatment of cancer can reduce the pain, mental and economic burden of patients, and strive for an early recovery of cancer patients. At present, most targeted drugs used for diagnosis and treatment are monoclonal fragments, which have poor tumor penetration ability and cannot be specifically captured by the monocyte-macrophage system. Peptides have the advantages of small amount, low immunogenicity, good tissue penetration ability and high affinity for tumor tissue. The research of targete...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06C07K1/16C07K1/13A61K49/14
Inventor 蒋孟军吴鹏西陈宏伟朱宝陈越新
Owner 蒋孟军
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