5-FU (5-Fluorouracil)

Catalog No.S1209 Batch:S120906

Technical Data

Formula

C₄H₃FN₂O₂

Molecular Weight

130.08

CAS No.

51-21-8

Solubility (25°C)*

In vitro

DMSO

100 mg/mL (768.75 mM)

Water

Insoluble

Ethanol

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	3.5mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 70 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 Corn oil	0.65mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 13 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

5-FU (5-Fluorouracil) is a DNA/RNA synthesis inhibitor, which interrupts nucleotide synthetic by inhibiting thymidylate synthase (TS) in tumor cells. Fluorouracil induces apoptosis and can be used in the treatment of HIV.

Targets

Thymidylate synthase ^[1]
(Tumor cells)

In vitro

Adrucil is an analogue of uracil with a fluorine atom at the C-5 position in place of hydrogen. It rapidly enters the cell using the same facilitated transport mechanism as uracil. Adrucil is converted intracellularly to several active metabolites: fluorodeoxyuridine monophosphate (FdUMP), fluorodeoxyuridine triphosphate (FdUTP) and fluorouridine triphosphate (FUTP). The Adrucil metabolite FdUMP binds to the nucleotide-binding site of TS, forming a stable ternary complex with the enzyme and CH2THF, thereby blocking binding of the normal substrate dUMP and inhibiting dTMP synthesis. Metabolite of Adrucil also can be misincorporated into DNA, leading to DNA strand breaks and cell death. The pro-apoptosis effects of Adrucil may be related to its activation of tumor suppressor p53. Loss of p53 function reduces cellular sensitivity to Adrucil. ^[1] Adrucil is able to inhibit the survival and induce apoptosis of a board range of cancer cells. Adrucil suppresses viabilities of the nasopharyngeal carcinoma cell line CNE2 and HONE1 ^[2], pancreatic cancer cell lines Capan-1 ^[3], and human colon carcinoma cell line HT-29 ^[4] with IC50 of 9 μg/mL, 3 μg/mL, 0.22 μM, 2.5 μM, respectively.

In vivo

Adrucil is widely used in the treatment of a range of cancers, including colorectal and breast cancers. ^[1] 100mg/kg Adrucil significantly suppresses tumor growth of murine colon carcinomas Colon 38 with tumor-doubling time (TD), growth-delay factor (GDF), and T/C of 26.5 days, 4.4, and 14%. ^[5]

Protocol (from reference)

Cell Assay:^{^[4]}	Cell lines Human colon carcinoma cell line HT-29 Concentrations ~25 μM Incubation Time 7 days Method Growth inhibition is measured after treatment of cells with Adrucil for 7 days in 96-well plates (4000 HT-29 cells/well in RPMI 1640 medium with 10% dialyzed fetal bovine serum); increasing concentrations of Adrucil are added after allowing for cell attachment overnight. At the end of incubation, cells are rinsed three times with phosphate-buffered saline (pH 7.4), fixed with 10% trichloroacetic acid for 60 min at 4 ℃, washed five times with deionized water, and stained with 0.4% sulforhoda-mine B solution for 15 min at room temperature. Unstained sulforhodamine B is removed by rinsing with 1% glacial acetic acid. Afterwards, stained cell proteins are dried and dissolved with 10 mM Tris-HCl. The optical density value is measured using a detector at 540 nm wavelength.
Animal Study:^{^[5]}	Animal Models Murine colon carcinomas Colon 38 Dosages 100 mg/kg Administration i.p. weekly

Cell Assay:^{^[4]}

Cell lines
Human colon carcinoma cell line HT-29
Concentrations
~25 μM
Incubation Time
7 days
Method
Growth inhibition is measured after treatment of cells with Adrucil for 7 days in 96-well plates (4000 HT-29 cells/well in RPMI 1640 medium with 10% dialyzed fetal bovine serum); increasing concentrations of Adrucil are added after allowing for cell attachment overnight. At the end of incubation, cells are rinsed three times with phosphate-buffered saline (pH 7.4), fixed with 10% trichloroacetic acid for 60 min at 4 ℃, washed five times with deionized water, and stained with 0.4% sulforhoda-mine B solution for 15 min at room temperature. Unstained sulforhodamine B is removed by rinsing with 1% glacial acetic acid. Afterwards, stained cell proteins are dried and dissolved with 10 mM Tris-HCl. The optical density value is measured using a detector at 540 nm wavelength.

Animal Study:^{^[5]}

Animal Models
Murine colon carcinomas Colon 38
Dosages
100 mg/kg
Administration
i.p. weekly

References

+ Expand

Customer Product Validation

: Data from [Data independently produced by Mol Cell Biochem, 2014, 10.1007/s11010-014-2253-6]

: Data from [Data independently produced by , , J Invest Dermatol, 2018, 138(8):1716-1725]

: Data from [Data independently produced by , , Eur Rev Med Pharmacol Sci, 2016, 20(9):1699-706.]

Selleck's 5-FU (5-Fluorouracil) has been cited by 285 publications

Modification of the telomerase gene with human regulatory sequences resets mouse telomeres to human length [ Nat Commun, 2025, 16(1):1211]	PubMed: 39905075
Prediction of Patient Drug Response via 3D Bioprinted Gastric Cancer Model Utilized Patient-Derived Tissue Laden Tissue-Specific Bioink [ Adv Sci (Weinh), 2025, 12(10):e2411769]	PubMed: 39748450
Inhibiting autophagy selectively prunes dysfunctional tumor vessels and optimizes the tumor immune microenvironment [ Theranostics, 2025, 15(1):258-276]	PubMed: 39744218
Targeting of the G9a, DNMT1 and UHRF1 epigenetic complex as an effective strategy against pancreatic ductal adenocarcinoma [ J Exp Clin Cancer Res, 2025, 44(1):13]	PubMed: 39810240
CXCR4-Targeted Ultrasound Microbubbles for Imaging and Enhanced Chemotherapy/Immunotherapy in Liver Cancer [ Acta Biomater, 2025, S1742-7061(25)00191-6]	PubMed: 40089129
The novel role of LCK and other PcDEGs in the diagnosis and prognosis of sepsis: Insights from bioinformatic identification and experimental validation [ Int Immunopharmacol, 2025, 149:114194]	PubMed: 39904039
Ruxolitinib as a novel therapeutic agent targeting mitochondrial function and chemo-resistance in nasopharyngeal carcinoma [ Biochem Biophys Res Commun, 2025, 753:151486]	PubMed: 39965265
Paired primary-metastasis patient-derived organoids and mouse models identify phenotypic evolution and druggable dependencies of peritoneal metastasis from appendiceal cancer [ bioRxiv, 2025, 2025.02.17.638725]	PubMed: 40027618
Enhanced fluorescence lifetime imaging microscopy denoising via principal component analysis [ bioRxiv, 2025, 2025.02.26.640419]	PubMed: 40060483
A novel DNA repair protein, N-Myc downstream regulated gene 1 (NDRG1), links stromal tumour microenvironment to chemoresistance [ bioRxiv, 2025, 2025.01.22.634323]	PubMed: 39896456

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SHIPPING AND STORAGE
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