Flucytosine
Based on 3 publication(s) in Google Scholar
Flucytosine (5-Fluorocytosine) is an antifungal compound with oral activity. Flucytosine is a widely used cytotoxic drug that, after further metabolism, produces fluorinated ribonucleotides and deoxyribonucleotides, inhibits DNA and protein synthesis, and has multiple effects such as inhibiting candida and candida neoplasm infection and producies cytotoxicity to cancer cells.
For research use only. We do not sell to patients.
- Purity : 99.97%
- CAS No.: 2022-85-7
- Formula: C4H4FN3O
- Molecular Weight:129.09
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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HY-90006
5-FluorouracilThymidylate Synthase Inhibitor -
HY-B0101
FluconazoleAntifungal Agent -
HY-B0221
Amphotericin BAntifungal Agent -
HY-17373
PosaconazoleAnti-fungal Agent -
HY-76200
VoriconazoleAntifungal Agent -
HY-17514
ItraconazoleAntifungal Agent -
HY-13637
GanciclovirAntiviral Agent -
HY-13259
MG-132Proteasome Inhibitor -
HY-B0105
KetoconazoleCYP3A4 Inhibitor -
HY-13553
AnidulafunginAntifungal Agent -
HY-17006
Caspofungin diacetateAntifungal Agent -
HY-B0139R
Flucytosine (Standard)Antifungal Agent
Publications Citing Use of MedChemExpress (MCE) Flucytosine
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Customer Validation & Images
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Others
All Antibiotic Isoforms
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Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| CCRF-CEM | IC50 |
>100 μM
Compound: 5-Fluorocytosine
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Cytotoxicity was determined in CEM cells, relative to RVT
Cytotoxicity was determined in CEM cells, relative to RVT
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[PMID: 15081000] |
| Vero | IC50 |
>100 μM
Compound: 5-Fluorocytosine
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Cytotoxicity was determined in Vero cells, relative to RVT
Cytotoxicity was determined in Vero cells, relative to RVT
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[PMID: 15081000] |
In Vitro
Flucytosine transfected CD-gene hMSC (CD-hMSC) effectively converts 5-FC into 5-FU, showing anti-cancer therapeutic potential[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Flucytosine (50, 75 mg/kg/ day, gavage, 3-30 days) combines with itraconazole (HY-17514) can effectively inhibit cryptococcus infection in hamsters[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-hMSC mice[2]
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Dosage:500 mg/kg
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Administration:i.v. for 7 days
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Result:Inhibited tumor volume and bodyweight.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2022-85-7
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Appearance Solid
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Molecular Weight 129.09
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Formula C4H4FN3O
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Color White to off-white
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SMILES
O=C1NC=C(F)C(N)=N1
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Synonyms
5-Fluorocytosine; NSC 103805; Ro 2-9915
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (3)
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Journal Impact Factor
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Most Recent
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Front Microbiol
Ketoconazole induces reversible antifungal drug tolerance mediated by trisomy of chromosome R in Candida albicans. [Abstract]2024 Jul 30:15:1450557. PMID: 39139375
Flucytosine purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2024 Jul 30:15:1450557. [Abstract]
We evaluated the resistance of wild-type strain SC5314 and two strains carrying ChrR trisomy and tetrasomy mutations, respectively, to a range of antifungal drugs, including azoles (clotrimazole and miconazole), echinocandins (caspofungin), and pyrimidines (5-Fluorocytosine).
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Appl Microbiol Biotechnol
Aloin remodels the cell wall of Candida albicans to reduce its hyphal virulence against oral candidiasis. [Abstract]2025 Jan 24;109(1):21. PMID: 39853490 -
Microbiol Spectr
Synergistic antifungal activity of minocycline as an effective augmenting agent of fluconazole against drug-resistant Candida tropicalis. [Abstract]2025 May 6;13(5):e0318524. PMID: 40162832
Solvent & Solubility
In Vitro:
DMSO : 16.67 mg/mL (129.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 6.67 mg/mL (51.67 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.67 mg/mL (12.94 mM); Clear solution
This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.67 mg/mL (12.94 mM); Clear solution
This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 8.67 mg/mL (67.16 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Handling Instructions (2659 KB)
References
[1]. Vermes A, et al. Flucytosine: a review of its pharmacology, clinical indications, pharmacokinetics, toxicity and drug interactions. J Antimicrob Chemother. 2000 Aug;46(2):171-9. [Content Brief]
[2]. You MH, et al. Cytosine deaminase-producing human mesenchymal stem cells mediate an antitumor effect in a mouse xenograft model. J Gastroenterol Hepatol. 2009 Aug;24(8):1393-400. [Content Brief]
[3]. Iovannitti C, et al. Itraconazole and flucytosine+itraconazole combination in the treatment of experimental cryptococcosis in hamsters. Mycoses. 1995 Nov-Dec;38(11-12):449-52. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 7.7465 mL | 38.7327 mL | 77.4653 mL | 193.6633 mL |
| 5 mM | 1.5493 mL | 7.7465 mL | 15.4931 mL | 38.7327 mL | |
| 10 mM | 0.7747 mL | 3.8733 mL | 7.7465 mL | 19.3663 mL | |
| 15 mM | 0.5164 mL | 2.5822 mL | 5.1644 mL | 12.9109 mL | |
| 20 mM | 0.3873 mL | 1.9366 mL | 3.8733 mL | 9.6832 mL | |
| 25 mM | 0.3099 mL | 1.5493 mL | 3.0986 mL | 7.7465 mL | |
| 30 mM | 0.2582 mL | 1.2911 mL | 2.5822 mL | 6.4554 mL | |
| 40 mM | 0.1937 mL | 0.9683 mL | 1.9366 mL | 4.8416 mL | |
| 50 mM | 0.1549 mL | 0.7747 mL | 1.5493 mL | 3.8733 mL | |
| DMSO | 60 mM | 0.1291 mL | 0.6455 mL | 1.2911 mL | 3.2277 mL |
| 80 mM | 0.0968 mL | 0.4842 mL | 0.9683 mL | 2.4208 mL | |
| 100 mM | 0.0775 mL | 0.3873 mL | 0.7747 mL | 1.9366 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Flucytosine Related Classifications
HY-B0139 Related Classifications
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