research use only

Flucytosine (5-Fluorocytosine) Fungal inhibitor

Cat.No.S1666

Flucytosine (5-Fluorocytosine) is an antifungal drug with IC50 of 0.93 μM in C. albicans.
Jump to

Quality Control

Batch: Purity: 99.93%
99.93

Solubility

In vitro
Batch:

DMSO : 13 mg/mL (100.7 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 7 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg
g
μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO
%
% Tween 80
% ddH2O
% DMSO
+
%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 129.09 Formula

C4H4FN3O

Storage (From the date of receipt)
CAS No. 2022-85-7 Download SDF Storage of Stock Solutions

Synonyms 5-FC, NSC 103805, Ro 2-9915 SMILES C1=NC(=O)NC(=C1F)N

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Features
First synthesized in 1957, and antifungal properties discovered in 1964.
In vitro
Flucytosine (5-Fluorocytosine) inhibits the growth of C. neoformans in Sabouraud's dextrose broth at concentrations ≥ 1.25 mg/L, and this compound at 50 mg/L causes a ~50% reduction in colony-forming unit (cfu) in the J774.16 killing assay with viability of J774.16 cells not affected measured by trypan blue exclusion. The combination of it and IgGl monoclonal antibody to Cryptococcus neoformans capsular glucuronoxylomannan is more effective in reducing the numbers of C. neoformans colony-forming units in vitro with J774.16 murine macrophage-like cells than either agent alone. The efficacy of 5FC in combination with amphotericin B (AB) and fluconazole (FCZ) is studied against 35 yeast isolates, of which the 5FC-FCZ combination is antagonistic against Candida species, but for some Candida isolates synergism is found.
Kinase Assay
Microdilution method
The culture media used are RPMI 1640 with glutamine, without bicarbonate and phenol red, buffered with morpholinopropanesulfonic acid (MOPS) (0.165 M, pH 7.0). Two-fold serial dilutions of Flucytosine (5-Fluorocytosine) (0.06-64 μg/mL) are prepared and dispensed in 50 uL aliquot, in flat-bottom 96-well assay plates which are kept frozen at -70 °C in sealed plastic bags until used. The inoculum is prepared spectrophotometrically and standardized to a concentration of 1.0-5.0 × 103 cfu per mL. A 50 μL volume of this suspension is used to inoculate each well containing 50 μL of the double concentration of this compound to be tested. Once inoculated, each well therefore contains 100 μL of broth favoured over 200 μL to facilitate the agitation of the plates prior to spectrophotometric reading. After an incubation period of 24 and 48 hours at 35 °C, the plates are agitated for 3 minutes at 900 r.p.m. with a shaker and the optical density of the growth in each well is determined with the use of an automatic plate reader set at 495 nm. The inhibitory concentration of IC50 is computed mathematically.
In vivo
Administration of Flucytosine (5-Fluorocytosine) in combination with monoclonal antibody 2H1 to A/JCr mice infected with C. neoformans significantly reduces lung but not brain cfu, which is more effective than either agent alone. The combination of intravenous it in 0.9% saline (NaCl) and amphotericin B (AmB) provides synergistic antifungal activity and is associated with a lower incidence of nephrotoxicity than with AmB treatment alone. Infusion of this compound (5-10 mg/kg/min) dissolved in 5% glucose into the renal artery of an in situ perfused kidney for 15 minutes increases renal blood flow (RBF) in the rat, and the renal vasodilatation persists for the duration of the infusion.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/1482135/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-05-28)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06264388 RECRUITING
High Grade Glioma; Anaplastic Astrocytoma
Ashish Shah
2024-05-01 PHASE2
NCT06666322 RECRUITING
Hiv; Cryptococcal Meningitis
David Boulware
2025-05-28 PHASE2; PHASE3
NCT06525389 NOT_YET_RECRUITING
Talaromycosis
Duke University
2026-09-01 PHASE3
NCT04105374 WITHDRAWN
Anaplastic Astrocytoma; Glioblastoma; Oligodendroglioma; Supratentorial Glioblastoma
NRG Oncology
2020-01-31 PHASE2; PHASE3
NCT06178627 UNKNOWN
Cryptococcal Meningitis; Antifungal Agents
Huashan Hospital
2023-08-13 PHASE4
NCT06414512 COMPLETED
Cryptococcal Meningitis
University of Minnesota
2024-04-09 PHASE2

Read more about Clinical Trials

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.