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Radioactive label tEB-TMTP1 compound and preparation method and application thereof

A technology for radiolabeling and compounding, applied in the field of radiolabeling compounds, to achieve mild reaction conditions, increase intake, and facilitate commercial application and clinical promotion

Active Publication Date: 2019-05-03
THE FIRST AFFILIATED HOSPITAL OF XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, there is currently no report on the combination of TMTP1 and tEB as a PET or SPECT diagnostic and therapeutic probe.

Method used

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  • Radioactive label tEB-TMTP1 compound and preparation method and application thereof
  • Radioactive label tEB-TMTP1 compound and preparation method and application thereof
  • Radioactive label tEB-TMTP1 compound and preparation method and application thereof

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Embodiment Construction

[0033] Below by embodiment the content of the present invention is specified:

[0034] (1) Preparation of DOTA-tEB-TMTP1 or NOTA-tEB-TMTP1

[0035] Put 0.1mmol of Fmoc-H-Gln(Trt)-2-Wang Resin resin into the reaction tube, add dichloromethane for swelling, then add 20% piperidine DMF solution for deprotection, add HBTU to activate the carboxyl group, and then add Fmoc- Arg(Pbf)-OH is coupled to complete a cycle of condensation, repeat the above operation, and add 0.4mmol of Fmoc-Val-OH, Fmoc-Val-OH, Fmoc-Asn(Trt)-OH, Fmoc-Gly-OH , Fmoc-Glu(OAll)-OH, DOTA-tris(tBu)easter or NOTA-bis(tBu)easter for condensation. Using 0.03mmol of Pd(OAc) 2 , 0.015 mmol PPh 3 , 1 mmol of N-methylmorpholine and 1 mmol of PhSiH 3 Deprotect the side chain OAll, then add 0.4mmol of EB dye, 0.4mmol of HBTU and 4mmol of DIPEA to condense under the conditions, stop the polypeptide reaction, take out the resin, put it into a sand core funnel, add dichloromethane to wash, blow After drying, add 2 mL c...

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Abstract

The invention discloses a radioactive label tEB-TMTP1 compound. Through modification with DOTA and NOTA bifunctional chelating agents, DOTA-tEB-TMTP1 and NOTA-tEB-TMTP1 are synthetized, radioactive metal nuclides of radioactive nuclides 68Ga, 64Cu and 177Lu and the like are respectively labelled, and a nuclear medicine diagnosis and treatment probe of specific target high-metastasis tumors is synthetized. The probe designed and synthesized from the radioactive label tEB-TMTP1 compound disclosed by the invention has two advantages that firstly the labelling steps are simple, higher labelling production rate is achieved, and a foundation is laid for clinical application; secondly, the obtained DOTA-tEB-TMTP1 probe and the obtained NOTA-tEB-TMTP1 probe have excellent pharmacokinetics nature,the half life of the DOTA-tEB-TMTP1 probe and the obtained NOTA-tEB-TMTP1 probe in bodies can be notably prolonged, the DOTA-tEB-TMTP1 probe and the obtained NOTA-tEB-TMTP1 probe can circulate in thebodies for a long term, tumor part ingestion is increased, and target treatment on high-metastasis tumors can be realized.

Description

technical field [0001] The invention relates to a radiolabeled tEB-TMTP1 compound and its preparation method and application, belonging to the field of radiolabeled compounds. Background technique [0002] According to statistics, the five-year survival rate of cancer patients in my country is only 20%, which is far lower than 70% in developed countries. Currently, surgery, radiotherapy and chemotherapy-based treatments can only remove existing cancer foci and kill some cancer cells, but cannot kill all cancer cells in the body, and the recurrence and metastasis rate within six months is as high as 69%. Therefore, it is very important to improve curative effect, control recurrence and metastasis, and reduce mortality for tumor treatment. [0003] Single photon emission computed tomography (SPECT) and positron emission computed tomography (PET) have shown their superiority in diagnosing and guiding the treatment of tumors and other diseases due to their characteristics of se...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06C07K1/04C07K1/06C07K1/13
CPCA61K45/06A61K49/0002A61P35/04A61K51/088A61K47/6455A61K51/0482A61K49/085
Inventor 李业森黄劲雄陈仔君林少唯吴华
Owner THE FIRST AFFILIATED HOSPITAL OF XIAMEN UNIV
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