1. Cell Cycle/DNA Damage
    Anti-infection
  2. Nucleoside Antimetabolite/Analog
    DNA/RNA Synthesis
    Bacterial
    CMV
    HSV
  3. Floxuridine

Floxuridine (Synonyms: 5-Fluorouracil 2'-deoxyriboside)

Cat. No.: HY-B0097 Purity: 98.89%
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Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis. Floxuridine has antiviral effects against HSV and CMV.

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Floxuridine Chemical Structure

Floxuridine Chemical Structure

CAS No. : 50-91-9

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Description

Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis[1][2]. Floxuridine has antiviral effects against HSV and CMV[3].

IC50 & Target[1][2][3]

DNA synthesis

 

Bacterial

 

HSV

 

CMV

 

In Vitro

Floxuridine (0-25 μM; 4-24 hours) is affectd by inhibitors of PARP and its sensitivity of ovarian cancer cells is enhanced. Co-exposed to FdUrd and the PARP inhibitor markedly increases killing cell numbers when its compare to treatment alone in ovarian cancer cells[1].
Floxuridine (300 μM; 4-24 hours) increases p-Chk1 and p-Chk2 in ovarian cancer cell lines. It may induce DNA damage and activate the ATM and ATR checkpoint signaling pathways[1].
Floxuridine (0-2.5 μM; 24 hours) causes a G1/S-phase arrest and following removal of the FdUrd, the G1/S-phase-arrested cells moved synchronously through S phase and into G2/M[1].
Floxuridine is against Mueller Hinton Broth and Tryptic Soy Broth with MIC values of 0.25 μM and 0.81 μM, respectively. It also reported to be a very potent inhibitor of staphylococcal growth (MIC, 0.025–0.00313 μM)[2].

Cell Viability Assay[1]

Cell Line: Ovarian cancer cells
Concentration: 0-25 μM
Incubation Time: 4, 8, 24 hours
Result: Was potentiated the sensitivity by  PARP inhibitors.

Western Blot Analysis[1]

Cell Line: OVCAR-8 and SKOV3ip cells
Concentration: 300 μM
Incubation Time: 4, 8, 24 hours
Result: Induced phosphorylation of Chk1 and Chk2 in two ovarian cancer cell lines

Cell Cycle Analysis[1]

Cell Line: A2780, SKOV3ip, OVCAR-5, and OVCAR-3 ovarian cancer cells
Concentration: 0.5, 1.0, 1.5, 2.0, and 2.5 μM
Incubation Time: 24 hours
Result: Induced cell arrest at G1/S-phase period.
In Vivo

Floxuridine  (intraperitoneal injection; 0.5-1.25 mg/kg; once per day for 7 days or single dose) is sufficient to show statistically significant protection against S. aureus infection at 0.5 mg/kg for 7 days. In addition, 1.25 mg/kg single administration of the compound shows statistically significant protection against S. aureus infection[2].

Animal Model: C57BL/6 mice injected with S. aureus[2]
Dosage: 0.5-1.25 mg/kg
Administration: once per day for 7 days or single dose
Result: Was a very potent inhibitor for S. aureus infection in vivo.
Clinical Trial
Molecular Weight

246.19

Formula

C₉H₁₁FN₂O₅

CAS No.

50-91-9

SMILES

OC[[email protected]@H]1[[email protected]](C[[email protected]](N2C(NC(C(F)=C2)=O)=O)O1)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 150 mg/mL (609.29 mM)

H2O : ≥ 50 mg/mL (203.10 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0619 mL 20.3095 mL 40.6190 mL
5 mM 0.8124 mL 4.0619 mL 8.1238 mL
10 mM 0.4062 mL 2.0310 mL 4.0619 mL
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: 98.89%

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Keywords:

Floxuridine5-Fluorouracil 2'-deoxyribosideNucleoside Antimetabolite/AnalogDNA/RNA SynthesisBacterialCMVHSVCytomegalovirusHerpes simplex virusS. aureuspolymeraseOncologyAntimetaboliteOvariancancercellsOVCAR-8SKOV3ipInhibitorinhibitorinhibit

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