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5-Fluorouracil

Catalog No. T0984 CAS 51-21-8

Synonyms: 5-FU, Fluorouracil, NSC 19893, 5-Fluoracil

5-Fluorouracil (5-FU) is a uracil analog, an inhibitor of DNA synthesis. 5-Fluorouracil has antitumor activity and affects pyrimidine synthesis through inhibition of thymidylate synthase. 5-Fluorouracil causes apoptosis and autophagy.

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5-Fluorouracil, CAS 51-21-8

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100 mg	In stock	$ 30.00
1 g	In stock	$ 48.00

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Purity: 100%

Purity: 99.83%

Purity: 99.56%

Purity: 98.77%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	5-Fluorouracil (5-FU) is a uracil analog, an inhibitor of DNA synthesis. 5-Fluorouracil has antitumor activity and affects pyrimidine synthesis through inhibition of thymidylate synthase. 5-Fluorouracil causes apoptosis and autophagy.
In vitro	METHODS: Human cardiomyocytes HCM, human umbilical vein endothelial cells HUVE, and human colon cancer cells HCT116 and HT29 were treated with 5-Fluorouracil (0.01-1000 µM) for 24-96 h, and the growth inhibition of the cells was detected by MTT. RESULTS: The EC50 of 5-Fluorouracil on HCM, HUVE, PHCT116 and HT29 cells were 4.866 μM, 3.832 μM, 13.72 μM and 106.8 μM, respectively, at 72 h. [1] METHODS: Smooth muscle cells were treated with 5-Fluorouracil (0.05-10 mM) for 24 h. Apoptosis was detected using Flow Cytometry. RESULTS: 5-Fluorouracil at concentrations of 0.1, 1, and 10 mM induced apoptosis in cultured smooth muscle cells after 24 h of treatment, and the apoptotic cells were detached from the culture dishes. [2] METHODS: Human colon cancer cells SW620 were incubated with 5-Fluorouracil (13 μg/mL) for 24-48 h. ALP activity was detected using an ALP detection kit. RESULTS: Alkaline phosphatase (ALP) has been used to monitor the differentiation effects of certain anticancer compounds. Untreated SW620 cells showed relatively low ALP activity, while in cells treated with 13 μg/ml 5-FU, ALP activity reached high levels in a time-dependent manner. [3]
In vivo	METHODS: To detect the antitumor activity in vivo, 5-Fluorouracil (10-40 mg/kg) was injected intraperitoneally once a day for ten days into mice bearing ascites hepatocellular carcinoma tumor H22. RESULTS: 5-Fluorouracil at 10 mg/kg inhibited tumor growth while maintaining immune function in mice. 5-Fluorouracil exerts low-dose, low-toxicity antitumor effects and stimulates the host immune system. [4] METHODS: To study 5-Fluorouracil-induced intestinal injury, 5-Fluorouracil (100-200 mg/kg) was administered as a single intraperitoneal injection to BALB/c mice. RESULTS: The body weight and diarrhea symptoms of 5-Fluorouracil-treated animals were significantly reduced in a dose-dependent manner. Occludin and claudin-1 protein expression was significantly reduced in the 5-Fluorouracil-treated group. 5-Fluorouracil-treated group showed significantly higher NF-κBp65 protein and TNF-α mRNA expression than the control group. NF-κBp65 protein and TNF-α mRNA expression were significantly higher in the 5-Fluorouracil treated group than in the control group. [5]
Cell Research	After a 7-day habituation period, the mice were divided into three groups (vehicle group, dextrin group, and ED group; n = 6 mice per group) that had the same mean body weight (time of grouping was designated as day 0). Then, mice were treated by tail vein injections from day 0 to 4; mice in the dextrin and ED groups received 40 mg/kg/day of 5- fluorouracil (5-FU) injection 250 mg, while mice in the vehicle group received 10 mL/kg/day physiological saline, which was equivalent to the dose of 5-FU. Additionally, twice a day from day 0 to 6, ED group mice received 1.6 kcal/0.8 mL/day ED administered orally, while mice in the vehicle and dextrin groups received dextrin containing the same amount of calories. Body weight and food consumption were measured before administration of 5-FU and ED on days 0 and 7. Food consumption was measured with respect to each group. Mice were accommodated individually in specially prepared polycarbonate cages, and two or more fresh stools per mouse were scored as follows: 0, the stools were not crushed when pushed by human fingers; 1, the stools were crushed, but the core remained when pushed by human fingers; 2, the stools were crushed and the core did not remain when pushed by human fingers; 3, the stools were crushed and stuck to the fingers when pushed by human fingers; 4, the stools lost their shape just from being touched. Autopsies were conducted on day 7. After bleeding, the large intestine (the colon and rectum) was taken, and the length was measured. The lumen was washed with physiological saline, the excess water was wiped off, and specimens were weighed. Section 3 cm distal from the center of the large intestine was fixed with formalin for histological evaluation. Salivary glands (the submandibular gland and sublingual gland) were collected and weighed. The collected salivary glands were fixed with formalin, and after the tissue sections were prepared, they were stained with hematoxylin and eosin [3].

Synonyms	5-FU, Fluorouracil, NSC 19893, 5-Fluoracil
Molecular Weight	130.08
Formula	C4H3FN2O2
CAS No.	51-21-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 1.3 mg/mL (10 mM)

DMSO: 13 mg/mL (100 mM)

References and Literature

1. Focaccetti C, et al. Effects of 5-fluorouracil on morphology, cell cycle, proliferation, apoptosis, autophagy and ROS production in endothelial cells and cardiomyocytes. PLoS One. 2. Filgueiras Mde C, et al. Effects of 5-fluorouracil in nuclear and cellular morphology, proliferation, cell cycle, apoptosis, cytoskeletal and caveolar distribution in primary cultures of smooth muscle cells. PLoS One. 2013 Apr 30;8(4):e63177. 3. Gao L, et al. Colon cancer cells treated with 5‑fluorouracil exhibit changes in polylactosamine‑type N‑glycans. Mol Med Rep. 2014 May;9(5):1697-702. 4. Cao Z, et al. Antitumor and immunomodulatory effects of low-dose 5-FU on hepatoma 22 tumor-bearing mice. Oncol Lett. 2014 Apr;7(4):1260-1264. 5. Song MK, et al. 5-Fluorouracil-induced changes of intestinal integrity biomarkers in BALB/c mice. J Cancer Prev. 2013 Dec;18(4):322-9. 6. Yin L, et al. Antitumor effects of oncolytic herpes simplex virus type 2 against colorectal cancer in vitro and in vivo. Ther Clin Risk Manag. 2017 Feb 7;13:117-130. 7. Kim W, Park C, Park J, et al. Pine needle hexane extract promote cell cycle arrest and premature senescence via p27 KIP1 upregulation gastric cancer cells[J]. Food Science and Biotechnology. 2020: 1-9. 8. Liu L, Liu S, Deng P, et al. Targeting the IRAK1-S100A9 Axis Overcomes Resistance to Paclitaxel in Nasopharyngeal Carcinoma[J]. Cancer Research.

Citations

1. Zhao X, Lian X, Xie J, et al.Accumulated cholesterol protects tumours from elevated lipid peroxidation in the microenvironment.Redox Biology.2023: 102678. 2. Zhu X, Huang N, Ji Y, et al.Brusatol induces ferroptosis in oesophageal squamous cell carcinoma by repressing GSH synthesis and increasing the labile iron pool via inhibition of the NRF2 pathway.Biomedicine & Pharmacotherapy.2023, 167: 115567. 3. Zhang S, Sun Y, Yao F, et al.Ginkgo Biflavones Cause p53 Wild-Type Dependent Cell Death in a Transcription-Independent Manner of p53.Journal of Natural Products.2023 4. Ouyang S, Li H, Lou L, et al. Inhibition of STAT3-ferroptosis negative regulatory axis suppresses tumor growth and alleviates chemoresistance in gastric cancer. Redox Biology. 2022: 102317 5. Zhao F, Huang Y, Zhang Y, et al. SQLE inhibition suppresses the development of pancreatic ductal adenocarcinoma and enhances its sensitivity to chemotherapeutic agents in vitro. Molecular Biology Reports. 2022: 1-9 6. Li Q, Lai Q, He C, et al. RUNX1 regulates the proliferation and chemoresistance of colorectal cancer through the Hedgehog signaling pathway. Journal of Cancer. 2021, 12(21): 6363-6371. 7. Liu L, Liu S, Deng P, et al. Targeting the IRAK1-S100A9 Axis Overcomes Resistance to Paclitaxel in Nasopharyngeal Carcinoma. Cancer Research. 2021 Mar 1;81(5):1413-1425. doi: 10.1158/0008-5472.CAN-20-2125. Epub 2021 Jan 5. 8. Xu X, Zhang S, Wang Y, et al. Virtual Screening Inhibitors of Ubiquitin-specific Protease 7 combining Pharmacophore Modeling and Molecular Docking. Molecular Informatics. 2022 9. Liu L, Liu S, Deng P, et al. Targeting the IRAK1–S100A9 Axis Overcomes Resistance to Paclitaxel in Nasopharyngeal Carcinoma. Cancer Research. 2021, 81(5): 1413-1425. 10. Luo X, Cai G, Guo Y, et al. Exploring Marine-Derived Ascochlorins as Novel Human Dihydroorotate Dehydrogenase Inhibitors for Treatment of Triple-Negative Breast Cancer. Journal of Medicinal Chemistry..

11. Lü Z, Li X, Li K, et al. Nitazoxanide and related thiazolides induce cell death in cancer cells by targeting the 20S proteasome with novel binding modes. Biochemical Pharmacology. 2022: 114913.

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Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Bioactive Compound Library Anti-Lung Cancer Compound Library Pediatric Drug Library Bioactive Compounds Library Max

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Keywords

5-Fluorouracil 51-21-8 Apoptosis Cell Cycle/Checkpoint DNA Damage/DNA Repair Metabolism Microbiology/Virology Proteases/Proteasome Nucleoside Antimetabolite/Analog HIV Protease Endogenous Metabolite DNA/RNA Synthesis 5-FU 5 Fluorouracil inhibit Fluorouracil NSC19893 Inhibitor 5Fluorouracil Human immunodeficiency virus HIV NSC 19893 5-Fluoracil NSC-19893 inhibitor

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