Compound for nanometer PET developer and its preparation method and use

A PET imaging agent and compound technology, applied in the field of nanomaterials, can solve the problems of unsatisfactory imaging effect of nano-PET imaging agent, difficult preparation of nano-PET imaging agent, low targeting ability, etc., and achieve objective and labeling conditions. Mild, high uptake effect

Active Publication Date: 2015-11-25
JIANGSU INST OF NUCLEAR MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The first technical problem to be solved by the present invention is the difficulty in preparation of nano-PET imaging agents in the prior art, low uptake rate in organisms, and low targeting, and then to provide a simple preparation, high uptake rate, and Higher tumor c

Method used

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  • Compound for nanometer PET developer and its preparation method and use
  • Compound for nanometer PET developer and its preparation method and use
  • Compound for nanometer PET developer and its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1: Synthesis of FB-CBT-KCRRVR

[0040] In this embodiment, the preparation method of FB-CBT-KCRRVR is as follows:

[0041] Dissolve 0.018mmol of the precursor substance CBT-KCRRVR in 5mL of phosphate buffer, then add 0.11mmol of SFB in 5mL of acetone solution, adjust the pH to 7.2, and react at 50°C for 8 hours to obtain the product.

[0042] The solution obtained by the above reaction was separated by HPLC, and the mixed solvent of acetonitrile and water added with 0.1V% trifluoroacetic acid was used as mobile phase, and gradient elution was carried out by a C18 chromatographic column (5 μm, 10mm×250mm). Increase from 30% to 70% within 30 minutes, keep the flow rate of the eluent at 3mL / min, collect the product, freeze-dry to obtain 0.012mmol of the product, and the product yield is 67%.

[0043] The product obtained above is confirmed by nuclear magnetic resonance and mass spectrometry, and the result is: 1 HNMR(d 4 -CD 3 OD,300MHz):8.63(s,1H),8.10(d,J=9.0...

Embodiment 2

[0045] Example 2: Synthesis of FB-CBT-KCRRVR

[0046] In this embodiment, the preparation method of FB-CBT-KCRRVR is as follows:

[0047] Dissolve 0.005mmol of the precursor substance CBT-KCRRVR in 5mL of water, then add 0.08mmol of SFB in 5mL of dimethylformamide solution, and adjust the pH of the reaction solution to 8.0 with 0.01M sodium carbonate buffer. React at 40°C for 5 hours to obtain.

[0048] The product was separated by HPLC using the same method as in Example 1 to obtain 0.0037 mmol of the product, and the product yield was 74%.

Embodiment 3

[0049] Example 3: Synthesis of FB-CBT-KCRRVR

[0050] In this embodiment, the preparation method of FB-CBT-KCRRVR is as follows:

[0051] Dissolve 0.0005 mmol of the precursor substance CBT-KCRRVR in 5 mL of water, then add 0.01 mmol of SFB in 5 mL of acetonitrile solution, and react at 10° C. for 24 hours to obtain the product.

[0052] Adopt the method HPLC separation product identical with embodiment 1, obtain product 0.00026mmol,

[0053] The product yield was 52%.

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Abstract

The invention discloses a compound for a nanometer PET developer. The compound A is shown in the structural formula (I). The compound A is a small molecule and can undergo a condensation reaction under the action of furin to produce a polymer large molecule. The polymer large molecule has good blood vessel and cell permeability, has a high uptake rate, can actively target an imaging zone, can self-assemble to form nanoparticles in the tumor zone, has high imaging sensitivity and good imaging effects, can be prepared simply, allows mild reaction conditions and can be used for high-expression furin tumor PET development.

Description

technical field [0001] The invention belongs to the field of nanomaterials, and in particular relates to a compound used as a nano-PET imaging agent and its preparation method and application. Background technique [0002] Positron emission tomography (PET) is one of the commonly used methods in the diagnosis of tumors. 11 C. 13 N. 15 O or 18 F and other radionuclide-labeled biologically active substances (such as glucose, amino acids, fats, antibodies, etc.) are used as imaging agents, and through the imaging of the accumulation and distribution of imaging agents in metabolism, the situation of life metabolic activities can be known, so that achieve the purpose of diagnosis. Positron tomography can not only quickly obtain multi-level tomographic images, realize three-dimensional whole-body scanning, and obtain three-dimensional quantitative results, but also dynamically observe the physiological changes of metabolites or drugs in vivo from the molecular level, and its p...

Claims

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Application Information

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IPC IPC(8): C07K7/06C07K1/02A61K51/08A61K101/02
Inventor 刘娅灵邹霈吴军王洪勇吴昊
Owner JIANGSU INST OF NUCLEAR MEDICINE
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