Fluorouracil (5-Fluoracil, 5-FU)

Description

Biological Activity

Protocol(Only for Reference)

Clinical Trial Information( data from http://clinicaltrials.gov)

Chemical Information

Cell Assay: ^[4]

Animal Study: ^[5]

References

貨號 Cat. No.: S1209
規格 Size: 5~200mg
品牌 Brand: Selleckchem

Fluorouracil (5-Fluoracil, 5-FU)

Catalog No.S12091 Product Citations

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

Size

Price

Stock

Quantity

10mM/1mLIn DMSO	USD 168	In stock	0 1 2 3 4 5 6 7 8 9 10
100mg	USD 185	In stock	0 1 2 3 4 5 6 7 8 9 10
200mg	USD 277	In stock	0 1 2 3 4 5 6 7 8 9 10

Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

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 â„ƒ, 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 Models	Murine colon carcinomas Colon 38
Dosages	100 mg/kg
Administration	i.p. weekly

NCT Number	Recruitment	Conditions	Sponsor /Collaborators	Start Date	Phases
NCT02015650	Not yet recruiting	Head and Neck Neoplasms	Medical University Innsbruck	2014-01	Phase 4
NCT02016417	Not yet recruiting	Nasopharyngeal Carcinoma	Cancer Hospital of Guangxi Medical University	2014-01	Phase 2
NCT01992705	Not yet recruiting	Resectable Pancreatic Cancer	University of Maryland	2014-01	Phase 0
NCT02017704	Not yet recruiting	Adenocarcinoma of the Prostate	Sidney Kimmel Comprehensive Cancer Center\|Nucletron	2014-02	Phase 2
NCT00960544	Not yet recruiting	Breast Cancer	M.D. Anderson Cancer Center\|Myriad Genetic Laboratories, Inc.	2014-03	Phase 2

Description

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

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.

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]

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

Molecular Weight (MW)	130.08
Formula	C₄H₃FN₂O₂
CAS No.	51-21-8

Storage	3 years -20â„ƒPowder
Storage	6 months-80â„ƒin DMSO
Syonnyms	5-FU, Carac, Efudex, Fluoroplex

Solubility (25°C) *	In vitro	DMSO	26 mg/mL (199 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	<1 mg/mL (<1 mM)
* <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.