A kind of fluorescent probe based on small molecule inhibitor and its preparation method and application
A technology of small molecule inhibitors and fluorescent probes, applied in fluorescence/phosphorescence, chemical instruments and methods, luminescent materials, etc., can solve problems that limit the wide application of nanobodies, untrue expression of target proteins, and affect the real function of proteins. Achieve the effects of easy quality control, short preparation time, and simple preparation method
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[0043] The present invention also provides a method for preparing a fluorescent probe based on a small molecule inhibitor, such as figure 1 shown, including the following steps:
[0044] Step 1: Derivatizing and modifying the small molecule inhibitor to obtain derivatives of the small molecule inhibitor;
[0045] Step 2: Linking the derivative of the small molecule inhibitor obtained in Step 1 with the linker molecule to obtain Product 2;
[0046] Step 3: react the product 2 obtained in step 2 with fluorescent dye molecules to obtain a fluorescent probe based on a small molecule inhibitor.
[0047] According to the present invention, it is first necessary to transform and modify the appropriate site of the small molecule inhibitor. The transformation process is a multi-step reaction, and the conditions are slightly different between different reactions. The preferred reaction solvent is N,N-dimethylformamide, acetonitrile , methanol or tetrahydrofuran, the reaction temperatu...
Embodiment 1
[0053] Embodiment 1: Preparation of gefitinib small molecule probe
[0054]
[0055] Step 1: Dissolve 500 mg of gefitinib in 60 ml of dichloromethane, slowly add 1.2 g of aluminum trichloride to the system in an ice-water bath, then remove the ice-water bath and heat at 60° C. for 16 hours with stirring. After the reaction was completed, it was cooled to 0° C., and saturated sodium bicarbonate was added to the system to quench the reaction. The organic phase was separated, and the aqueous phase was extracted three times with dichloromethane. The organic phases were combined, dried over anhydrous sodium sulfate, filtered, and concentrated to obtain 80 mg of product 1.
[0056] Step 2: Dissolve 45 mg of product 1 in 1 ml of acetonitrile, add 45 mg of PEG-linked molecules and 43 mg of potassium carbonate into the system under stirring, and then raise the temperature to 50° C. for 10 hours. After the reaction, it was cooled to room temperature, diluted with ethyl acetate, wash...
Embodiment 2
[0061] Example 2: Preparation of Tariquina Small Molecule Probe
[0062]
[0063] Step 1: Dissolve 1 g of 4-nitrophenethyl bromide and 1.0 g of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline hydrochloride in 20 ml of DMF Afterwards, 670 mg of potassium carbonate and 145 mg of potassium iodide were added to the system respectively, and the temperature was raised to 70° C. and stirred for 16 hours. After the reaction, it was cooled to room temperature, diluted with water, extracted three times with ethyl acetate, and the organic phases were combined. The organic phase was washed three times with saturated sodium chloride, dried over anhydrous sodium sulfate, filtered, and the initial product was concentrated. The product was separated by column to obtain 800 mg of compound 4.
[0064] Step 2: 800 mg of compound 4 was dissolved in 10 ml of methanol, and then 80 mg of palladium-carbon catalyst was added to the system, replaced with nitrogen three times and then replaced with hy...
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