Fiacitabine
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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.
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- Pureza: 99.27%
- No. CAS: 69123-90-6
- Fòrmula: C9H11FIN3O4
- Peso molecular:371.10
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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DNA Polymerase |
HSV-1 |
HSV-2 |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 2.2.15 | EC50 |
5 μM
Compound: 35
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Anti hepatitis-B virus activity was evaluated in 2.2.15 cells.
Anti hepatitis-B virus activity was evaluated in 2.2.15 cells.
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[PMID: 8709113] |
| HepG2 2.2.15 | IC50 |
>200 μM
Compound: 35
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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
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Cytotoxic concentration required to inhibit NC-37 cells by 50%
Cytotoxic concentration required to inhibit NC-37 cells by 50%
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10.1016/S0960-894X(01)80146-3 |
| NC-37 | EC50 |
0.1 μg/mL
Compound: 3
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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
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10.1016/S0960-894X(01)80146-3 |
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.
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Cell Line:Uninfected Vero, WI-38, and NC-37 cells
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Concentration:0.1 μM, 1 μM, 10 μM, 100 μM
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Incubation Time:4 days
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 69123-90-6
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Appearance Solid
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Peso molecular 371.10
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Fòrmula C9H11FIN3O4
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Color White to off-white
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SMILES
OC[C@@H]1[C@@H](O)[C@H](F)[C@H](N(C=C2I)C(N=C2N)=O)O1
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Synonyms
NSC 382097; FIAC; FOAC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1].
Allaudeen HS, et al. Selective inhibition of DNA replication in herpes simplex virus infected cells by 1-(2'-deoxy-2'-fluoro-beta-D-arabinofuranosyl)-5-iodocytosine. J Biol Chem. 1982 Oct 25;257(20):11879-82. PMID: 6288702.
[Content Brief]
[2]. Lopez C, et al. 2'-fluoro-5-iodo-aracytosine, a potent and selective anti-herpesvirus agent. Antimicrob Agents Chemother. 1980;17(5):803-806. [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, 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 |
Fiacitabine Related Classifications
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