1. Anti-infection Cell Cycle/DNA Damage
  2. HSV EBV DNA/RNA Synthesis
  3. Fiacitabine

Fiacitabine  (Synonyms: NSC 382097; FIAC; FOAC)

Cat. No.: HY-50735 Purity: 99.27%
Handling Instructions Technical Support

Fiacitabine (NSC 382097; FIAC; FOAC) is a potent and highly selective anti-herpesvirus agent. Fiacitabine acts as an inhibitor of HSV DNA polymerase, with a Ki of 0.26 μM for HSV-1 and 0.42 μM for HSV-2, respectively. Fiacitabine can be efficiently phosphorylated by thymidine kinase encoded by the virus itself to generate FIACTP, an active triphosphate metabolite. Fiacitabine is applicable to research related to herpesvirus infections.

For research use only. We do not sell to patients.

Fiacitabine

Fiacitabine Chemical Structure

CAS No. : 69123-90-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
1 mg In-stock
5 mg In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Fiacitabine (NSC 382097; FIAC; FOAC) is a potent and highly selective anti-herpesvirus agent. Fiacitabine acts as an inhibitor of HSV DNA polymerase, with a Ki of 0.26 μM for HSV-1 and 0.42 μM for HSV-2, respectively. Fiacitabine can be efficiently phosphorylated by thymidine kinase encoded by the virus itself to generate FIACTP, an active triphosphate metabolite. Fiacitabine is applicable to research related to herpesvirus infections[1][2].

IC50 & Target[1]

DNA Polymerase

 

HSV-1

 

HSV-2

 

Cellular Effect
Cell Line Type Value Description References
HepG2 2.2.15 EC50
5 μM
Compound: 35
Anti hepatitis-B virus activity was evaluated in 2.2.15 cells.
Anti hepatitis-B virus activity was evaluated in 2.2.15 cells.
[PMID: 8709113]
HepG2 2.2.15 IC50
> 200 μM
Compound: 35
The growth inhibition activity for the compound was evaluated in 2.2.15 cells.
The growth inhibition activity for the compound was evaluated in 2.2.15 cells.
[PMID: 8709113]
NC-37 CC50
63 μg/mL
Compound: 3
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
0.1 μg/mL
Compound: 3
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
In Vitro

FIACTP potently and competitively inhibits purified HSV-1 DNA polymerase (Ki = 0.26 μM), HSV-2 DNA polymerase (Ki = 0.42 μM), human leukemic leukocyte DNA polymerase α (Ki = 2.7 μM), human leukemic leukocyte DNA polymerase β (Ki = 7.9 μM), and EBV DNA polymerase (Ki = 32.2 μM) relative to dCTP, with HSV-1 DNA polymerase being the most sensitive target[1].
FIAC (2.5 μg/mL-12.5 μg/mL; 24 h) preferentially inhibits viral DNA synthesis rather than cellular DNA synthesis in HSV-1-infected Vero cells[1].
Fiacitabine (18-20 h) potently inhibits the replication of wild-type HSV-1 strains Patton, HFEM, MacIntyre, 2931 and wild-type HSV-2 strains 333, G in Vero cells[2].
Fiacitabine (78 μM; 18-20 h) inhibits the replication of thymidine kinase-negative mutant HSV-1 in Vero cells. The 90% effective dose at 18-20 h post-treatment is 78 μM, and this mutant strain is approximately 8000-fold less sensitive to it than wild-type HSV-1[2].
Fiacitabine (0.1-100 μM; 4 days) exhibits only extremely low cytotoxicity in uninfected Vero, WI-38 and NC-37 cells, with IC50 values of 5 μM, 4 μM and 10 μM respectively after 4 days of treatment[2].
Fiacitabine inhibits plaque formation of the HZV Ellen strain in WI-38 cells, with an IC50 of 0.01 μM[2].

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

Cell Cytotoxicity Assay[2]

Cell Line: Uninfected Vero, WI-38, and NC-37 cells
Concentration: 0.1 μM, 1 μM, 10 μM, 100 μM
Incubation Time: 4 days
Result: Reduced Vero cell proliferation by 50% at 5 μM after 4 days of culture.
Reduced WI-38 cell proliferation by 50% at 4 μM after 4 days of culture.
Reduced NC-37 cell proliferation by 50% at 10 μM after 4 days of culture.
Inhibited WI-38 cell proliferation by 98% at 100 μM in the absence of deoxycytidine.
Clinical Trial
Molecular Weight

371.10

Formula

C9H11FIN3O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC[C@@H]1[C@@H](O)[C@H](F)[C@H](N(C=C2I)C(N=C2N)=O)O1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 37 mg/mL (99.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6947 mL 13.4735 mL 26.9469 mL
5 mM 0.5389 mL 2.6947 mL 5.3894 mL
View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.27%

References

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6947 mL 13.4735 mL 26.9469 mL 67.3673 mL
5 mM 0.5389 mL 2.6947 mL 5.3894 mL 13.4735 mL
10 mM 0.2695 mL 1.3473 mL 2.6947 mL 6.7367 mL
15 mM 0.1796 mL 0.8982 mL 1.7965 mL 4.4912 mL
20 mM 0.1347 mL 0.6737 mL 1.3473 mL 3.3684 mL
25 mM 0.1078 mL 0.5389 mL 1.0779 mL 2.6947 mL
30 mM 0.0898 mL 0.4491 mL 0.8982 mL 2.2456 mL
40 mM 0.0674 mL 0.3368 mL 0.6737 mL 1.6842 mL
50 mM 0.0539 mL 0.2695 mL 0.5389 mL 1.3473 mL
60 mM 0.0449 mL 0.2246 mL 0.4491 mL 1.1228 mL
80 mM 0.0337 mL 0.1684 mL 0.3368 mL 0.8421 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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