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Molecular probe and preparation method and application thereof

A technology of molecular probes and targeting molecules, applied in chemical instruments and methods, pharmaceutical formulations, in vivo radioactive preparations, etc., can solve false positives, false negatives in disease diagnosis, single-target molecular imaging cannot accurately reflect biological processes in vivo, etc. problem, to achieve the effect of high imaging contrast and good stability

Inactive Publication Date: 2014-03-19
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] The occurrence and development of many diseases are not caused by changes in a single indicator, so single-target molecular imaging cannot accurately reflect biological processes in vivo, which can easily lead to false positives or false negatives in disease diagnosis

Method used

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  • Molecular probe and preparation method and application thereof
  • Molecular probe and preparation method and application thereof
  • Molecular probe and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1 Preparation of Molecular Probe D1

[0043] 1) Under nitrogen protection, the substance Diamsar (20 mg, 63.7 μmol) was dissolved in acetone-methanol mixed solvent (wherein by volume ratio, V 丙酮 :V 甲醇 =1:2), then added p-bromophenethylamine (60mg, 300μmol), reacted at 60-70℃ for 10h, cooled to room temperature, purified by HPLC preparative chromatography, and freeze-dried to obtain the product A1 (25.3mg, 72 %, the retention time is 8.7min). A1 electrospray mass spectrometer ESI-MS result: m / z=552.8 (A1 molecular formula is C 30 h 52 N 10 , the theoretical value is 552.8).

[0044]

[0045]2) Dissolve 4-(N-maleimidomethyl)cyclohexane-1-carboxylic acid sulfosuccinimidyl ester sodium salt (Sulfo-SMCC; 43.6 mg, 100 μmol) in EDC (28.8 mg , 150μmol) / NHS (16.2mg, 140μmol) mixed solution (EDC: 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride; NHS: N-hydroxysuccinimide ), using 0.1mol L -1 Dilute hydrochloric acid to adjust the pH of the solution t...

Embodiment 2

[0051] Example 2 Preparation of Molecular Probe E2

[0052] 1) Under the protection of nitrogen, dissolve the substance Diamsar (20 mg, 63.7 μmol) in a mixed solvent of tetrahydrofuran and methanol (wherein, V 四氢呋喃 :V 甲醇 =1:2), then added β-alanine (35.6mg, 400μmol), reacted at 55°C for 12-20h, cooled to room temperature, purified by HPLC preparative chromatography, and freeze-dried to obtain the product A2 (23.8mg , 82%, retention time is 7.5min). A2 electrospray mass spectrometer ESI-MS result: m / z=456.4 (A2 molecular formula is C 20 h 44 N 10 o 2 , theoretical m / z value is 456.4).

[0053]

[0054] 2) Dissolve the obtained product A2 (5.5mg, 10μmol) in 3mL boric acid buffer (pH 8.5); then add 4-(N-maleimidomethyl)cyclohexane-1-carboxylic acid Sodium salt of succinimide ester (Sulfo-SMCC; 34.88 mg, 80 μmol) was dissolved in EDC (20.16 mg, 90 μmol) / NHS (10.5 mg, 90 μmol) mixed solution (EDC: 1-(3-dimethylaminopropyl )-3-ethylcarbodiimide hydrochloride; NHS: N-hydro...

Embodiment 3

[0062] The preparation of embodiment 3 molecular probe G3, H3

[0063] 1) Under the protection of nitrogen, dissolve the compound of formula II (Diamsar: 20 mg, 63.7 μmol) in a mixed solvent of tetrahydrofuran and acetone (wherein by volume, V 四氢呋喃 :V 丙酮 =2:1), then Fmoc-protected 3,4,5-trihydroxy-2-carboxy-7-aminopyran (structural formula below) (85.75 mg, 200 μmol) was dissolved in EDC (13.44 mg, 70 μmol) with HOBT (70μmol) mixed solution, mix the two solutions, react at room temperature for 2-4 hours, add morpholine (100μmol), and then stir at 50-60℃ for 8-9 hours, and finally use 0.1mol L -1 Dilute hydrochloric acid solution to adjust the pH to 5-7, react at 40-50°C for 2-3 hours, cool to room temperature, prepare HPLC for separation and purification, and lyophilize to obtain product A3 (33.5mg, 76%, retention time: 6.9min) . A3 electrospray mass spectrometer ESI-MS result: m / z=692.8 (A3 molecular formula is C 28 h 56 N 10 o 10 , theoretical m / z value is 692.8).

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Abstract

The invention discloses a molecular probe, and a preparation method and application thereof. A series of dual-mode single-target and single-mode dual-target molecular imaging probes can be obtained by connecting different arm molecules. The obtained probes are good in stability and high in development contrast. Active targeting to a diseased region by the molecular probes is achieved through the connected targeted molecules and signal molecules by researching the synthesized molecular probes, and application of the molecular probe in preparation of a drug for diagnosis and treatment of different tumor diseases is achieved by connecting different targeted molecules.

Description

technical field [0001] The invention relates to an imaging molecular probe, in particular to a class of coupled isotopes 64 Cu, linking infrared dye molecules as signal molecules, using antibodies or antibody fragments as targeting molecules, forming dual-mode or dual-target molecular probes and their preparation methods and applications. Background technique [0002] Molecular imaging is a cutting-edge discipline that integrates advanced imaging technology with molecular biology technology, computer information processing technology and other disciplines to image at the molecular level. Compared with traditional medical imaging technology, molecular imaging can understand the occurrence and development of diseases and their mechanisms at the molecular level, and provide molecular level information for early clinical diagnosis, treatment and disease research. One of the keys to molecular imaging is specific molecular probes, so the design and synthesis of molecular probes h...

Claims

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Application Information

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IPC IPC(8): A61K51/00A61K49/00C09K11/06C07K16/12C07K7/52
Inventor 王怡红李新辈钱坤魏术海
Owner SOUTHEAST UNIV
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