Fluorouracil (5-Fluorouracil, 5-FU)
For research use only.
Catalog No.S1209 Synonyms: NSC 19893
CAS No. 51-21-8
Fluorouracil (5-Fluorouracil, 5-FU, NSC 19893) 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.
Selleck's Fluorouracil (5-Fluorouracil, 5-FU) has been cited by 85 publications
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|Description||Fluorouracil (5-Fluorouracil, 5-FU, NSC 19893) 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.|
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.  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 , pancreatic cancer cell lines Capan-1 , and human colon carcinoma cell line HT-29  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.  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%. |
-  Longley DB, et al. Nat Rev Cancer, 2003, 3(5), 330-338.
-  Qin L, et al. Biochem Biophys Res Commun, 2008, 371(3), 531-535.
-  Shi X, et al. Oncology, 2002, 62(4), 354-362.
|In vitro||DMSO||26 mg/mL (199.87 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
For best results, use promptly after mixing.
* 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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
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Molecular Weight Calculator
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04158349||Recruiting||Drug: Oxaliplatin|Drug: mFOLFIRI||Colorectal Cancer|Appendiceal Cancer|Peritoneal Carcinoma||University of Utah||June 11 2020||Phase 1|
|NCT04370418||Not yet recruiting||Drug: short course chemo-radiation with 5-fluorouracil||Neo-adjuvant Short Course Chemo-radiation in Locally Advanced Cancer Rectum||Assiut University||May 2020||--|
|NCT04274933||Recruiting||Drug: Venetoclax|Drug: Capecitabine||Breast Cancer|Cancer||AbbVie||May 21 2020||Phase 1|
|NCT04274790||Not yet recruiting||Procedure: Scheduled and planned surgery||Cancer of Colon|Metastasis to Liver||Centre Leon Berard||March 1 2020||--|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
I was wondering if the product #s1209 (5-fluorouracil) is suitable to inject into mice ?
S1209 is suitable to inject (I.P.) into mice as indicating in this paper: http://www.ncbi.nlm.nih.gov/pubmed/8995503.