Fluorouracil (5-Fluoracil, 5-FU)

Catalog No.S1209 Synonyms: NSC 19893

Molecular Weight(MW): 130.08

Fluorouracil (5-Fluoracil, 5-FU) is a DNA/RNA synthesis inhibitor, which interrupts nucleotide synthetic by inhibiting thymidylate synthase (TS) in tumor cells.

Cited by 13 Publications

Cancer Res, 2017, 77(18):5039-5053

PubMed: 28716899 ( click the link to review the publication )

J Invest Dermatol, 2018, 138(8):1716-1725

PubMed: 29550418 ( click the link to review the publication )

J Exp Clin Cancer Res, 2018, 37(1):151

PubMed: 30005681 ( click the link to review the publication )

Cell Physiol Biochem, 2018, 46(4):1365-1380

PubMed: 29689552 ( click the link to review the publication )

Neuroendocrinology, 2018, 106(1):58-73

PubMed: 28226315 ( click the link to review the publication )

Neuroendocrinology, 2018, 106(4):335-351

PubMed: 28968593 ( click the link to review the publication )

J Proteomics, 2014, 113:326-36

PubMed: 25451013 ( click the link to review the publication )

PLoS One, 2017, 12(5):e0178375

PubMed: 28542590 ( click the link to review the publication )

PLoS One, 2013, 8(1):e54595

PubMed: 23355882 ( click the link to review the publication )

Mol Cell Biochem, 2014, 10.1007/s11010-014-2253-6

PubMed: 25348361 ( click the link to review the publication )

Oncol Lett, 2018, 15(6):9385-9391

PubMed: 29946371 ( click the link to review the publication )

Eur Rev Med Pharmacol Sci, 2016, 20(9):1699-706

PubMed: 27212159 ( click the link to review the publication )
Sci Rep, 2016, 6:29382

PubMed: 27387652 ( click the link to review the publication )

3 Customer Reviews

Quantitative RT-PCR analysis for mTOR levels in ASZ001 cells treated with ITRA, VISMO, or 5-FU. Data represent the mean ± SD of three independent experiments. * p < 0.05, compared to nontreated controls; ns, statistically not significant.

J Invest Dermatol, 2018, 138(8):1716-1725. Fluorouracil (5-Fluoracil, 5-FU) purchased from Selleck.

DNA-PKcs suppression mediated ROS production and GSH content in HepG2 cells exposed to CDDP and 5-Fu. a DNA-PKcs inhibition promoted ROS production in HepG2 cells treated with indicated concentrations of CDDP and 5-Fu. DCFH-DA fluorescent analysis was performed to assess the ROS level. Data presented were mean ?SD of three independent experiments.

Mol Cell Biochem 2014 10.1007/s11010-014-2253-6. Fluorouracil (5-Fluoracil, 5-FU) purchased from Selleck.
EdU staining of RBE cells treated with OSI-027 (6.25 μM) and/or 5-FU (6.25 μg/mL) was performed by using Click-iT EdU Imaging Kit. The percentages of EdU-positive cells have been provided in the right panel.

Eur Rev Med Pharmacol Sci, 2016, 20(9):1699-706.. Fluorouracil (5-Fluoracil, 5-FU) purchased from Selleck.

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Biological Activity

Description

Fluorouracil (5-Fluoracil, 5-FU) is a DNA/RNA synthesis inhibitor, which interrupts nucleotide synthetic by inhibiting thymidylate synthase (TS) in tumor cells.

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.

Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
MCF-7	NFrqc4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVG3NuKhcMLi	NHLxcFBKSzVyPUKwJO69\y:vTB?=	NEm0bJIzPDB7NUG3Oi=>
HT-29	M2m0cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MoXsO\|LDqGkEoB?=	M3\ITmlEPTB-IEK1JO69\y:vTB?=	NH\KZWMzPDB7NUG3Oi=>
HL-60	M1TBdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MoXpO\|LDqGkEoB?=	MX\JR\|UxRThwNkCxJO69\y:vTB?=	NHHVTngzPDB7NUG3Oi=>
NCI-H292	M3zX[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M1SyWFczyqCqwrC=	M1XKb2lEPTB-IEK1JO69\y:vTB?=	Mn\ENlQxQTVzN{[=

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p53 / PUMA / c-PARP; PubMed: 25965911 Oncotarget (A) HCT-116 cells were treated with various doses of 5-FU for 24 hours (B) HCT-116 cells were treated with 200 uM 5-FU, then harvested at different time points after stimulation. The expression of p53, PUMA, cleaved PARP and P-Akt(S473) were detected by western blotting in different conditions.	25965911
Immunofluorescence	caveolin-3; PubMed: 23646193 PLoS One Cells were stained with an antibody against caveolin-3 (green) and with DAPI (blue). (A) control cells (top images), 10 mM 5-FU (middle images), 50 mM 5-FU (bottom images). Merged images are shown at the right of each panel. phospho-histone H3 ; PubMed: 23646193 PLoS One Cells were grown for 24 h, treated with 5-FU and stained with an anti-phospho-histone H3 antibody (red) and with DAPI (blue). (A) control cells, (B) 0.1 mM 5-FU and (C) 1 mM 5-FU. p65 / p-p65(Ser536) / p53 / p-p53(Ser15); PubMed: 24587255 PLoS One E–H, Immunocytochemistry of p65 and p53 induction and localization by 5-FU treatment for the indicated cell lines. p65 (red), phosphor-p65 (Ser536; red), p53 (green), phospho-p53 (Ser15; red), and DAPI (blue) staining of the nucleus without (control) and with 5-FU treatment. Sox2 / Oct4 / Nanog / ABCG2; PubMed: 27009861 Oncotarget (A) Immunofluorescence staining of Sox2, Oct4 and Nanog in HBE cells with or without 5-FU treatment. In untreated HBE cells, few Sox2, Oct4 or Nanog-positive cells were observed. After 5-FU treatment, the number of Sox2, Oct4 or Nanog-positive cells increased remarkably. Nuclei were counterstained with DAPI (blue). (B) Immunofluorescence staining of ABCG2 in HBE cells with or without 5-FU treatment. β-catenin; PubMed: 30111797 Exp Mol Med Immunofluorescence detection of β-catenin in HCT-8 cells. Scale bar, 20 μm. non-phospho β-catenin; PubMed: 28588704 Oncol Lett Effect of enhanced WNT signaling in Ell3 OE cells. Localization of non-phosphorylated β-catenin was analyzed by immunocytochemical staining in (A) control MCF-7 and (B) Ell3 OE treated with various 5-FU concentrations.	23646193 24587255 27009861 30111797 28588704
Growth inhibition assay	Cell viability; PubMed: 25965911 Oncotarget Cells viability was analyzed using Cell Counting Kit-8 at 0, 3, 6, 12 and 24 hours after (A) 50, 100, 200, or 400 uM 5-FU treatment in HCT116 cells. Cell proliferation; PubMed: 30250641 Oncotarget (A) Cell proliferation assay with resveratrol in HCT116. Cells were treated with resveratrol at 0 ~ 200 μM for 72 hours and applied to MTS assay. (B) HCT116 cells were treated with 5-FU at 0~200 μM for 72 hours. (C)HCT116 cells were treated with resveratrol at 0 ~ 200 μM combined with 5-FU at 10 μM for 72 hours and applied to MTS assay. (D) DLD1 cell proliferation assay with resveratrol at 0 ~ 200 μM for 72 hours. (E) DLD1 cells were treated with 5-FU at 0~ 200 μM for 72 hours. (F) DLD1 cells were treated with resveratrol combined with 5-FU at 10 μM for 72 hours. Error bars represent standard deviation.	25965911 30250641

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

Cell Research:^[4]	+ Expand 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. (Only for Reference)
Animal Research:^[5]	+ Expand Animal Models: Murine colon carcinomas Colon 38 Formulation: PBS Dosages: 100 mg/kg Administration: i.p. weekly (Only for Reference)

Cell Research:^[4]

+ Expand

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.
(Only for Reference)

Animal Research:^[5]

+ Expand

Animal Models: Murine colon carcinomas Colon 38
Formulation: PBS
Dosages: 100 mg/kg
Administration: i.p. weekly
(Only for Reference)

References

+ Expand

Solubility (25°C)

In vitro	DMSO	26 mg/mL (199.87 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): saline (warming) For best results, use promptly after mixing.	10mg/mL

* 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.

Chemical Information Download Fluorouracil (5-Fluoracil, 5-FU) SDF

Molecular Weight	130.08
Formula	C₄H₃FN₂O₂
CAS No.	51-21-8
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	NSC 19893

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-03-27)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03196180	Not yet recruiting	High Grade Cervical Intraepithelial Neoplasia\|p16 Positive Neoplastic Cells Present	National Cancer Institute (NCI)	July 31 2019	Phase 1
NCT03196180	Not yet recruiting	High Grade Cervical Intraepithelial Neoplasia\|p16 Positive Neoplastic Cells Present	National Cancer Institute (NCI)	July 31 2019	Phase 1
NCT03883919	Not yet recruiting	Pancreatic Cancer\|Pancreas Cancer\|Cancer of the Pancreas	Washington University School of Medicine\|Ipsen	June 30 2019	Phase 1
NCT03883919	Not yet recruiting	Pancreatic Cancer\|Pancreas Cancer\|Cancer of the Pancreas	Washington University School of Medicine\|Ipsen	June 30 2019	Phase 1
NCT03784326	Not yet recruiting	Clinical Stage II Esophageal Adenocarcinoma AJCC v8\|Clinical Stage II Gastroesophageal Junction Adenocarcinoma AJCC v8\|Clinical Stage IIA Esophageal Adenocarcinoma AJCC v8\|Clinical Stage IIA Gastroesophageal Junction Adenocarcinoma AJCC v8\|Clinical Stage IIB Esophageal Adenocarcinoma AJCC v8\|Clinical Stage IIB Gastroesophageal Junction Adenocarcinoma AJCC v8\|Clinical Stage III Esophageal Adenocarcinoma AJCC v8\|Clinical Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IB Esophageal Adenocarcinoma AJCC v8\|Pathologic Stage IB Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IC Esophageal Adenocarcinoma AJCC v8\|Pathologic Stage IC Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage II Esophageal Adenocarcinoma AJCC v8\|Pathologic Stage II Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IIA Esophageal Adenocarcinoma AJCC v8\|Pathologic Stage IIA Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IIB Esophageal Adenocarcinoma AJCC v8\|Pathologic Stage IIB Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage III Esophageal Adenocarcinoma AJCC v8\|Pathologic Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IIIA Esophageal Adenocarcinoma AJCC v8\|Pathologic Stage IIIA Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IIIB Esophageal Adenocarcinoma AJCC v8\|Pathologic Stage IIIB Gastroesophageal Junction Adenocarcinoma AJCC v8	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	May 31 2019	Early Phase 1
NCT03775265	Not yet recruiting	Bladder Carcinoma Infiltrating the Muscle of the Bladder Wall\|Bladder Urothelial Carcinoma\|Stage II Bladder Cancer AJCC v8\|Stage III Bladder Cancer AJCC v8\|Stage IIIA Bladder Cancer AJCC v8	National Cancer Institute (NCI)	May 9 2019	Phase 3

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Question 1:
I was wondering if the product #s1209 (5-fluorouracil) is suitable to inject into mice ?
Answer:
S1209 is suitable to inject (I.P.) into mice as indicating in this paper: http://www.ncbi.nlm.nih.gov/pubmed/8995503.

DNA/RNA Synthesis Signaling Pathway Map

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Fluorouracil (5-Fluoracil, 5-FU)

Cited by 13 Publications

3 Customer Reviews

Purity & Quality Control

Choose Selective DNA/RNA Synthesis Inhibitors

Biological Activity

Protocol

References

Solubility (25°C)

Chemical Information Download Fluorouracil (5-Fluoracil, 5-FU) SDF

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Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The Serial Dilution Calculator Equation

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Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-03-27)

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Frequently Asked Questions

DNA/RNA Synthesis Signaling Pathway Map

Related DNA/RNA Synthesis Products0

Choose Your Country or Region

By Signaling Pathways

By product type

Fluorouracil (5-Fluoracil, 5-FU)

Cited by 13 Publications

3 Customer Reviews

Purity & Quality Control

Choose Selective DNA/RNA Synthesis Inhibitors

Biological Activity

Protocol

References

Solubility (25°C)

Chemical Information Download Fluorouracil (5-Fluoracil, 5-FU) SDF

Bio Calculators

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Dilution Calculator

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

The Serial Dilution Calculator Equation

Serial Dilutions

Computed Result

Molecular Weight Calculator

Total Molecular Weight: g/mol

Instructions to calculate molar mass (molecular weight) of a chemical compound:

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-03-27)

Tech Support

Frequently Asked Questions

DNA/RNA Synthesis Signaling Pathway Map

Related DNA/RNA Synthesis Products0

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)