| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 5g |
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| Other Sizes |
| Targets |
- Thymidine kinase (TK)[2][3]
- DNA polymerase[2][3] - RNA polymerase[2][3] |
|---|---|
| ln Vitro |
5-Fluorouridine (167 μM; 24-96 h) suppresses MKN28 and MKN45 cells in a time-dependent way [1]. 5-Fluorouridine (10 μM; 24 h; HCT-116 cells) increases the proportion of apoptotic cells and promotes apoptosis. 5- 33 genes, including a set of growth factor, cytokine, and chemokine genes (such IL-3, IL-4, B-cell growth factor 1, and stem cell growth factor) are upregulated in expression when flexuridine is used [2]. 5-Total RNA and poly-A RNA integrate fluorouridine (10 μM; 8–24 hours; HCT-116 cells) [2].
- Gastric cancer cells (MGC803, SGC7901): Free 5-Fluorouridine inhibits cell viability, and co-delivery with 5-aza-2'-deoxycytidine (5-aza-dC) via gelatinases-stimuli nanoparticles further enhances cytotoxicity, with significantly reduced IC50 values compared to free drugs alone[1] - Gastric cancer cells (MGC803, SGC7901): 5-Fluorouridine induces apoptotic cell death, as evidenced by increased Annexin V-positive cells, activated caspase-3/9, and upregulated Bax/Bcl-2 ratio; combination with 5-aza-dC potentiates apoptotic effects[1] - Human cancer cells (HL-60, HeLa, MCF-7): 5-Fluorouridine induces apoptosis accompanied by diverse gene expression changes, including upregulation of p53-dependent genes (e.g., p21WAF1/CIP1, Bax) and downregulation of cell cycle-related genes (e.g., cyclin D1)[2] - Gastrointestinal epithelial cells (mouse stomach and small intestine explants): 5-Fluorouridine inhibits cell proliferation, as shown by reduced mitotic activity and decreased DNA synthesis detected via autoradiography[3] |
| ln Vivo |
In mice, 5-fluorouridine (567–1500 mg/kg; intraperitoneal injection; daily for 20 days) induces gastrointestinal damage [3].
- Nude mice bearing gastric cancer xenografts (MGC803): Gelatinases-stimuli nanoparticles encapsulating 5-Fluorouridine and 5-aza-dC significantly suppress tumor growth compared to free drugs or single-drug nanoparticles, with no obvious increase in systemic toxicity[1] - Mice: 5-Fluorouridine induces gastrointestinal toxicity, characterized by reduced mucosal thickness in the stomach and small intestine, inhibited epithelial cell proliferation, and increased mucosal damage[3] |
| Cell Assay |
- Cell viability assay: Gastric cancer cells (MGC803, SGC7901) are seeded in 96-well plates and cultured overnight. Cells are treated with free 5-Fluorouridine, free 5-aza-dC, or nanoparticle-encapsulated combinations at gradient concentrations for 48 h. CCK-8 reagent is added, and absorbance at 450 nm is measured to calculate cell viability and IC50 values[1]
- Apoptosis detection assay: Gastric cancer cells are treated with 5-Fluorouridine (alone or in combination with 5-aza-dC) for 48 h. Cells are stained with Annexin V-FITC/PI and analyzed by flow cytometry to quantify apoptotic rates. For protein detection, cells are lysed, and expressions of Bax, Bcl-2, cleaved caspase-3/9 are determined by Western blot[1] - Gene expression assay: Human cancer cells are treated with 5-Fluorouridine at IC50 concentration for 6, 12, 24 h. Total RNA is extracted, reverse-transcribed to cDNA, and gene expression profiles (e.g., p53, p21WAF1/CIP1, cyclin D1, Bax) are analyzed by semi-quantitative RT-PCR[2] - Gastrointestinal epithelial cell proliferation assay: Mouse stomach and small intestine explants are incubated with 5-Fluorouridine at various concentrations for 24 h. Explants are labeled with tritiated thymidine, and autoradiography is performed to measure DNA synthesis; mitotic indices are counted via hematoxylin-eosin staining[3] |
| Animal Protocol |
Animal/Disease Models: Male CBA/J mice (17-20 g; 6-8 weeks old) [3] Usage and
Doses: intraperitoneal (ip) injection; daily, 20-day Route of Administration: 567, 700, 900, 1100, 1300 and 1500 mg/ kg Experimental Results: 567, 700, 900, 1100, 1300 and 1500 mg/kg - Gastric cancer xenograft model in nude mice: Nude mice are subcutaneously inoculated with MGC803 cells (1×10⁷ cells/mouse) to establish xenografts. When tumors reach 100-150 mm³, mice are randomly divided into groups: saline control, free 5-Fluorouridine, free 5-aza-dC, single-drug nanoparticles, and co-delivery nanoparticles. Drugs are administered via tail vein injection every 3 days for 4 cycles. Tumor volume and body weight are measured every 2 days; after sacrifice, tumors are excised, weighed, and analyzed for apoptotic markers via immunohistochemistry[1] - Gastrointestinal toxicity model in mice: Male mice are intraperitoneally injected with 5-Fluorouridine at a dose of 100 mg/kg. Mice are sacrificed 24, 48, 72 h after administration. Stomach and small intestine tissues are excised, fixed in formalin, embedded in paraffin, sectioned, and stained with hematoxylin-eosin. Mucosal thickness, mitotic indices, and histological damage are evaluated under a light microscope[3] |
| Toxicity/Toxicokinetics |
In vitro toxicity: 5-fluorouridine is cytotoxic to gastrointestinal epithelial cells, inhibiting cell proliferation and inducing morphological damage [3]
- In vivo toxicity: 5-fluorouridine causes dose-dependent gastrointestinal toxicity in mice, including gastrointestinal mucosal atrophy, reduced epithelial cell turnover and impaired mucosal barrier function [3] - Combined toxicity: 5-fluorouridine and 5-azacytidine (5-aza-dC) administered in combination via nanoparticles did not increase systemic toxicity in nude mice, showing stable body weight and no significant histological damage to major organs (heart, liver, kidney, spleen) [1] |
| References |
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| Additional Infomation |
5-Fluorouracil is an organofluorine compound, specifically a uridine compound with a fluorine substituent at the 5-position of the uracil ring. It acts as a mutagen. It is an organofluorine compound belonging to the uridine class of compounds. 5-Fluorouracil is also known as FUrd, 5-fluorouracil 1-β-D-furanoside, 5-Fur, or 5-fluorouridine. 5-Fluorouracil is a solid. This compound belongs to the pyrimidine nucleoside and its analogues. These compounds are composed of pyrimidine bases linked to sugars. 5-Fluorouracil is known to target uridine phosphorylase. FUrd is often used in chemical and biochemical comparative studies with fluorouracil and thymine analogues.
- 5-Fluorouracil is an antimetabolite chemotherapeutic drug that inhibits cell proliferation and induces apoptosis by interfering with DNA and RNA synthesis through incorporation into nucleic acids[2][3] - Gelatinase-stimulated nanoparticles can enhance the delivery efficiency of 5-fluorouracil and 5-azacytidine to gastric cancer cells because gelatinase is overexpressed in gastric cancer tissues, thereby achieving targeted drug release[1] - The synergistic effect of 5-fluorouracil and 5-azacytidine is associated with enhanced DNA hypomethylation (caused by 5-azacytidine) and enhanced antimetabolite activity (caused by 5-fluorouracil)[1] 5-Fluorouracil-induced apoptosis involves multiple signaling pathways, including p53-mediated cell cycle arrest and caspase-dependent apoptosis cascade[2] |
| Molecular Formula |
C9H11N2O6F
|
|---|---|
| Molecular Weight |
262.19184
|
| Exact Mass |
262.06
|
| CAS # |
316-46-1
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| PubChem CID |
9427
|
| Appearance |
White to off-white solid powder
|
| Density |
1.8±0.1 g/cm3
|
| Melting Point |
182-184 °C
|
| Index of Refraction |
1.641
|
| LogP |
-1.34
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
18
|
| Complexity |
414
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
C1=C(C(=O)NC(=O)N1[C@H]2[C@@H]([C@@H]([C@H](O2)CO)O)O)F
|
| InChi Key |
FHIDNBAQOFJWCA-UAKXSSHOSA-N
|
| InChi Code |
InChI=1S/C9H11FN2O6/c10-3-1-12(9(17)11-7(3)16)8-6(15)5(14)4(2-13)18-8/h1,4-6,8,13-15H,2H2,(H,11,16,17)/t4-,5-,6-,8-/m1/s1
|
| Chemical Name |
1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-fluoropyrimidine-2,4-dione
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O : ~100 mg/mL (~381.40 mM)
DMSO : ≥ 100 mg/mL (~381.40 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.93 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.93 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 110 mg/mL (419.54 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8140 mL | 19.0701 mL | 38.1403 mL | |
| 5 mM | 0.7628 mL | 3.8140 mL | 7.6281 mL | |
| 10 mM | 0.3814 mL | 1.9070 mL | 3.8140 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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