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5-fluorouracil derivatives, 5-fluorouracil immunogens, antibodies for immunogens and 5-fluorouracil detection kit

A technology of fluorouracil and derivatives, applied in immunoglobulins, animal/human peptides, animal/human proteins, etc., can solve the problems of not meeting the needs of clinical testing and not being suitable for clinical applications.

Inactive Publication Date: 2015-04-01
苏州博源医疗科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, traditional methods such as high performance liquid chromatography (HPLC) are mainly used to monitor the blood concentration of 5-FU at home and abroad, but these methods are not suitable for clinical application. Although latex-enhanced immune turbidimetry has been used in China, it can be applied The 5-fluorouracil assay kit for biochemical analyzers is on the market, but it is far from meeting the growing demand for clinical testing
At present, there is a lack of 5-fluorouracil detection reagents with good stability, high sensitivity and strong specificity in the market, especially high-quality automated detection reagents. 5-fluorouracil assay reagents for automatic biochemical analyzers have become a hot spot in the in vitro diagnostic reagent industry at home and abroad

Method used

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  • 5-fluorouracil derivatives, 5-fluorouracil immunogens, antibodies for immunogens and 5-fluorouracil detection kit
  • 5-fluorouracil derivatives, 5-fluorouracil immunogens, antibodies for immunogens and 5-fluorouracil detection kit
  • 5-fluorouracil derivatives, 5-fluorouracil immunogens, antibodies for immunogens and 5-fluorouracil detection kit

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1: Synthesis and structure confirmation of 5-fluorouracil derivatives

[0040] The chemical structure of the 5-fluorouracil derivative used in the following examples is shown in formula (IV):

[0041]

[0042] The synthetic route of 5-fluorouracil derivative shown in this formula (IV) is as follows:

[0043]

[0044] The synthetic steps of the 5-fluorouracil derivative shown in formula (IV) are as follows:

[0045] 1) Weigh 5g (38.5mmol) of compound 15-fluorouracil, 6.95g (50.3mmol) of 2-bromoacetic acid and 4.48g (80.0mmol) of KOH and dissolve them in 50mL of water, then stir the solution at 60°C overnight; The reactant was adjusted to pH=5 with HCl, and then filtered; the filtered solid was washed with water and then vacuum-dried to obtain 2 g of 5-fluorouracil derivative as a white solid, with a yield of 27.6%.

[0046] 2) Structural identification of the purified product obtained above:

[0047] a. Using Varian III plus 300MHz to scan the NMR spectr...

Embodiment 2

[0050] Example 2: Synthesis of BSA-5-fluorouracil derivative immunogen

[0051] BSA-5-fluorouracil immunogen is composed of bovine serum albumin (Bovine Serum Albumin, BSA) and 5-fluorouracil derivative-(CH 2 ) n-COO-group connected, in this embodiment, take n=1 as an example to describe the synthesis method of the immunogen in detail, the specific steps are as follows:

[0052] Bovine serum albumin (200mg) was dissolved in 50ml 0.2M, in the phosphate buffer of pH 8.5;

[0053] Add the following chemicals into a small beaker and stir to dissolve: 200 mg of synthetic 5-fluorouracil derivative, 3.5 ml of dimethylformamide (dimethylformamide, DMF), 3.5 ml of ethanol, 7.0 ml of 10 mM potassium phosphate buffer at pH 5.0, 220mg 1-ethyl-3-(-3-dimethylaminopropyl) carbodiimide, 50mg N-hydroxysulfosuccinimide (N-hydroxysulfosuccinimide, Sulfo-NHS), these chemicals at room temperature Stir and dissolve for 30 minutes;

[0054] The dissolved solution was added dropwise to the BSA sol...

Embodiment 3

[0055] Example 3: Synthesis of KLH-5-fluorouracil derivative immunogen

[0056] KLH-5-fluorouracil immunogen is composed of hemocyanin (KLH) and 5-fluorouracil derivative-(CH 2 )n-COO-group connected, in this embodiment, take n=2 as an example to describe the synthesis method of the immunogen in detail, the specific steps are as follows:

[0057] Hemocyanin (180mg) was dissolved in 60ml 0.15M, in the phosphate buffer of pH 8.7;

[0058] Add the following chemicals into a small beaker and stir to dissolve: 200 mg of synthetic 5-fluorouracil derivatives, 3.5 ml of dimethylformamide (dimethylformamide, DMF), 2.8 ml of ethanol, 6.3 ml of 12 mM potassium phosphate buffer at pH 4.8, 160mg 1-ethyl-3-(-3-dimethylaminopropyl) carbodiimide, 40mg N-hydroxysulfosuccinimide (N-hydroxysulfosuccinimide, Sulfo-NHS), put these chemicals at room temperature Stir and dissolve for 25 minutes;

[0059] The dissolved solution was added dropwise to the KLH solution and stirred overnight at 2°C to...

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Abstract

The invention provides 5-fluorouracil derivatives, 5-fluorouracil immunogens, antibody for the immunogens, and a 5-fluorouracil detection kit. The 5-fluorouracil derivatives provided by the invention have a structure shown in a formula (I) as shown in the specification, wherein R is -(CH2)n-COO- and n is an integer between 1 and 20. The 5-fluorouracil derivatives with the structural formula are combined with a specific carrier, so that the prepared 5-fluorouracil immunogens have high immunogenicity; and the antibodies generated by an animal immunized with the immunogens have relatively high sensitivity and specificity, and have high specific combining ability with 5-fluorouracil. Through use of a homogeneous enzyme immune detection technology, high-flux and fast detection of 5-fluorouracil by an full automatic biochemical analyzer can be achieved; and the detection is convenient to operate, high in sensitivity, high in specificity, accurate in result and the like; the 5-fluorouracil detection cost can be effectively reduced; and clinical promotion and application are facilitated.

Description

technical field [0001] The invention relates to the field of immune detection, in particular to a 5-fluorouracil derivative, a 5-fluorouracil immunogen and its antibody, and a 5-fluorouracil detection kit. Background technique [0002] 5-fluorouracil (5-Fluorouracil, 5-FU), its structural formula is shown in formula (Ⅲ): [0003] [0004] 5-fluorouracil, an analog of uracil, is one of the most important chemotherapeutic drugs in cancer treatment. It is usually used in chemotherapy regimens for various cancers such as colon cancer, rectal cancer, gastric cancer, breast cancer and pancreatic cancer. The drug has definite curative effect. It can inactivate the thymine synthase that synthesizes DNA, and can also be incorporated into RNA to cause lethal synthesis. The metabolism and clearance of 5-FU in the body are related to many factors, and the pharmacokinetics has nonlinear and The characteristics of saturability, toxicity and efficacy have high intra- and inter-individ...

Claims

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Application Information

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IPC IPC(8): C07D239/553C07K14/765C07K14/795C07K14/47C07K1/107C07K16/44
CPCC07D239/553C07K14/47C07K14/765C07K14/795C07K16/44C07K19/00
Inventor 虞留明邓拥军陈丽峰陆丽华余琳
Owner 苏州博源医疗科技有限公司
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