5-FU (5-Fluorouracil)

Catalog No.S1209 Batch:S120905

Technical Data

Formula	C₄H₃FN₂O₂
Molecular Weight	130.08	CAS No.	51-21-8
Solubility (25°C)*	In vitro	DMSO	26 mg/mL (199.87 mM)
		Water	10 mg/mL warmed with 50ºC water bath (76.87 mM)
		Ethanol	Insoluble
* <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.)

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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

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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 238 publications

Synergistic antitumor activity between HER2 antibody-drug conjugate and chemotherapy for treating advanced colorectal cancer [ Cell Death Dis, 2024, 15(3):187]	PubMed: 38443386
A functional personalised oncology approach against metastatic colorectal cancer in matched patient derived organoids [ NPJ Precis Oncol, 2024, 8(1):52]	PubMed: 38413740
Novel dual action PARP and microtubule polymerization inhibitor AMXI-5001 powerfully inhibits growth of esophageal carcinoma both alone and in combination with radiotherapy [ Am J Cancer Res, 2024, 14(1):378-389]	PubMed: 38323288
Molecular Mechanisms of Drug Resistance And Strategies of Sensitization in Breast Cancer [ Frontiers, 2024, 10.3389/978-2-8325-4184-5]	PubMed: none
ST6GAL1 is associated with poor response to chemoradiation in rectal cancer [ Neoplasia, 2024, 51:100984]	PubMed: 38467087
The ribosomal protein L22 binds the MDM4 pre-mRNA and promotes exon skipping to activate p53 upon nucleolar stress [ bioRxiv, 2024, 10.1101/2023.12.29.573614]	PubMed: none
The ribosomal protein L22 binds the MDM4 pre-mRNA and promotes exon skipping to activate p53 upon nucleolar stress [ bioRxiv, 2024, 10.1101/2023.12.29.573614]	PubMed: none
Codon-specific KRAS mutations predict survival benefit of trifluridine/tipiracil in metastatic colorectal cancer [ Nat Med, 2023, 29(3):605-614]	PubMed: 36864254
Lysine butyrylation of HSP90 regulated by KAT8 and HDAC11 confers chemoresistance [ Cell Discov, 2023, 9(1):74]	PubMed: 37460462
Colorectal Cancer Organoid-Stroma Biobank Allows Subtype-Specific Assessment of Individualized Therapy Responses [ Cancer Discov, 2023, 13(10):2192-2211]	PubMed: 37489084

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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