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 259 publications

YTHDF2 in peritumoral hepatocytes mediates chemotherapy-induced antitumor immune responses through CX3CL1-mediated CD8+ T cell recruitment [ Mol Cancer, 2024, 23(1):186]	PubMed: 39237909
AMG 193, a Clinical Stage MTA-Cooperative PRMT5 Inhibitor, Drives Antitumor Activity Preclinically and in Patients With MTAP-Deleted Cancers [ Cancer Discov, 2024, 10.1158/2159-8290.CD-24-0887]	PubMed: 39282709
mTORC2-driven chromatin cGAS mediates chemoresistance through epigenetic reprogramming in colorectal cancer [ Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0]	PubMed: 39080411
The MYCN oncoprotein is an RNA-binding accessory factor of the nuclear exosome targeting complex [ Mol Cell, 2024, S1097-2765(24)00285-5]	PubMed: 38703770
Personalized drug screening using patient-derived organoid and its clinical relevance in gastric cancer [ Cell Rep Med, 2024, 5(7):101627]	PubMed: 38964315
DPP9 regulates NQO1 and ROS to promote resistance to chemotherapy in liver cancer cells [ Redox Biol, 2024, 75:103292]	PubMed: 39094401
Modulation of NLRP3 inflammasome-related-inflammation via RIPK1/RIPK3-DRP1 or HIF-1α signaling by phenothiazine in hypothermic and normothermic neuroprotection after acute ischemic stroke [ Redox Biol, 2024, 73:103169]	PubMed: 38692093
Intracellular cartilage oligomeric matrix protein augments breast cancer resistance to chemotherapy [ Cell Death Dis, 2024, 15(7):480]	PubMed: 38965233
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 senescence restriction point acting on chromatin integrates oncogenic signals [ Cell Rep, 2024, 43(4):114044]	PubMed: 38568812

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SHIPPING AND STORAGE
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