Art. -Nr.: HY-118122

Fialuridine

(Synonyms: FIAU; DRG-0098; NSC 678514)

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Fialuridine (FIAU), a nucleoside analog, is a HSV-1 and HSV-2 inhibitor with K_is of 0.14 μM and 0.95 μM, respectively. Fialuridine shows anti-orthopoxvirus and anti-hepatitis B virus (HBV) activities. Fialuridine inhibits duck HBV DNA replication with IC₅₀ values of 0.075 μM and 156 μM in human hepatoma cells and in chicken liver cells, respectively.

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Reinheit: 99.98%
CAS. Nr.: 69123-98-4
Formel: C₉H₁₀FIN₂O₅
Molecular Weight:372.09

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Fialuridine Chemical Structure

CAS. Nr.: 69123-98-4

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle HSV Isoform-spezifische Produkte anzeigen :

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
NC-37	CC₅₀	6.7 μg/mL Compound: 4	Cytotoxic concentration required to inhibit NC-37 cells by 50% Cytotoxic concentration required to inhibit NC-37 cells by 50%	10.1016/S0960-894X(01)80146-3
NC-37	EC₅₀	0.06 μg/mL Compound: 4	Concentration required to reduce HSV-1 (KOS strain) induced cytopathogenicity in NC-37 cells Concentration required to reduce HSV-1 (KOS strain) induced cytopathogenicity in NC-37 cells	10.1016/S0960-894X(01)80146-3
RG2	CC₅₀	80 μM Compound: FIAU	Cytotoxicity against RG2 cells after 72 hrs by MTT assay Cytotoxicity against RG2 cells after 72 hrs by MTT assay	[PMID: 18800764]
Sf21	IC₅₀	>1000 μM Compound: Fialuridine	Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]
Sf21	IC₅₀	>1000 μM Compound: Fialuridine	Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]

In Vitro

Fialuridine against Vaccinia and Cowpox viruses in HFF cells with EC₅₀ values of 1.5 and 0.2 μM, respectively^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

DNA is obtained from tissues of dogs administered Fialuridine (FIAU) at 0, 1, 2, or 3 mg/kg of body weight per day for 90 days, monkeys administered Fialuridine at 0 or 25 mg/kg per day for 30 days, and rats administered Fialuridine at 0, 255, or 510 mg/kg per day for 70 days. Fialuridine incorporation was observed in all species. In the rat, Fialuridine is incorporated into DNA of all tissues examined, with highest concentrations in the liver followed by jejunum, spleen, and heart. Fialuridine is also incorporated into sperm DNA^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 69123-98-4
Appearance Solid
Molecular Weight 372.09
Formel C₉H₁₀FIN₂O₅
Color White to off-white
SMILES

O[C@H]1[C@H](F)[C@H](N2C(NC(C(I)=C2)=O)=O)O[C@@H]1CO
Synonyms

FIAU; DRG-0098; NSC 678514
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (268.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6875 mL

13.4376 mL

26.8752 mL

5 mM

0.5375 mL

2.6875 mL

5.3750 mL

10 mM

0.2688 mL

1.3438 mL

2.6875 mL

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.72 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.72 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.72 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Mansuri MM, et al. 1-(2-Deoxy-2-fluoro-beta-D-arabinofuranosyl)-5-ethyluracil. A highly selective antiherpes simplex agent. J Med Chem. 1987 May;30(5):867-71. [Content Brief]

[2]. Mark N Prichard, et al. Orthopoxvirus targets for the development of antiviral therapies. Curr Drug Targets Infect Disord. 2005 Mar;5(1):17-28. [Content Brief]

[3]. Staschke KA, et al. The in vitro anti-hepatitis B virus activity of FIAU [1-(2'-deoxy-2'-fluoro-1-beta-D-arabinofuranosyl-5-iodo)uracil] is selective, reversible, and determined, at least in part, by the host cell. Antiviral Res. 1994 Jan;23(1):45-61. [Content Brief]

[4]. Richardson FC, et al. Fialuridine accumulates in DNA of dogs, monkeys, and rats following long-term oral administration. Proc Natl Acad Sci U S A. 1994 Dec 6;91(25):12003-7. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6875 mL	13.4376 mL	26.8752 mL	67.1880 mL
	5 mM	0.5375 mL	2.6875 mL	5.3750 mL	13.4376 mL
	10 mM	0.2688 mL	1.3438 mL	2.6875 mL	6.7188 mL
	15 mM	0.1792 mL	0.8958 mL	1.7917 mL	4.4792 mL
	20 mM	0.1344 mL	0.6719 mL	1.3438 mL	3.3594 mL
	25 mM	0.1075 mL	0.5375 mL	1.0750 mL	2.6875 mL
	30 mM	0.0896 mL	0.4479 mL	0.8958 mL	2.2396 mL
	40 mM	0.0672 mL	0.3359 mL	0.6719 mL	1.6797 mL
	50 mM	0.0538 mL	0.2688 mL	0.5375 mL	1.3438 mL
	60 mM	0.0448 mL	0.2240 mL	0.4479 mL	1.1198 mL
	80 mM	0.0336 mL	0.1680 mL	0.3359 mL	0.8399 mL
	100 mM	0.0269 mL	0.1344 mL	0.2688 mL	0.6719 mL

Keywords

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Fialuridine

Anti-Infection Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Antiviral Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Reprogramming Compound Library

Nucleotide Compound Library

Anti-Lung Cancer Compound Library

Drug-Induced Liver Injury (DILI) Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Liver Cancer Compound Library

Rare Diseases Drug Library

Anti-Orthopoxvirus Compound Library

Mitochondrial Toxicity Compound Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle HSV Isoform-spezifische Produkte anzeigen

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Fialuridine

Anti-Infection Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Antiviral Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Reprogramming Compound Library

Nucleotide Compound Library

Anti-Lung Cancer Compound Library

Drug-Induced Liver Injury (DILI) Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Liver Cancer Compound Library

Rare Diseases Drug Library

Anti-Orthopoxvirus Compound Library

Mitochondrial Toxicity Compound Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle HSV Isoform-spezifische Produkte anzeigen

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Fialuridine Related Classifications

HY-118122 Related Classifications