| Size | Price | Stock | Qty |
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| 1g |
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| Other Sizes |
| Targets |
DNA synthesis; viral DNA polymerase. As a halogenated pyrimidine nucleoside analog, 1-(2-Deoxy-2-fluoro-beta-D-arabinofuranosyl)uracil is incorporated into DNA, disrupting nucleic acid synthesis. The compound targets rapidly dividing cells and has antiviral properties against HSV-1 and HSV-2. It is a purine nucleoside analog with broad antitumor activity.
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| ln Vitro |
1-(2-Deoxy-2-fluoro-beta-D-arabinofuranosyl)uracil demonstrates activity as a nucleoside analog in cellular assays. It has antitumor activity against chronic lymphocytic leukemia, non-Hodgkin's lymphoma, and acute myeloid leukemia. It also has antiviral properties against herpes simplex virus 1 and 2. Detailed IC50 values have not been disclosed.
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| ln Vivo |
In vivo activity of 1-(2-Deoxy-2-fluoro-beta-D-arabinofuranosyl)uracil has been demonstrated in clinical settings for the treatment of CLL, non-Hodgkin's lymphoma, and AML. Its antiviral properties against HSV have also been observed in vivo. The compound's in vivo efficacy supports its therapeutic applications.
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| Enzyme Assay |
In vitro assays for nucleoside analogs involve measuring inhibition of DNA synthesis using radiolabeled thymidine incorporation. The compound is incubated with cancer cells at varying concentrations, and incorporation of labeled nucleosides is measured. Antiviral assays are performed in virus-infected cells. Cell viability is assessed by MTT or CellTiter-Glo assays.
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| Cell Assay |
Cells (e.g., leukemia cell lines or HSV-infected cells) are cultured and treated with the compound at concentrations typically ranging from 0.1–100 μM for 24–72 hours. DNA synthesis inhibition is measured by BrdU incorporation. Cell viability is assessed by standard assays. Viral replication is measured by qPCR or plaque assays.
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| Animal Protocol |
In vivo animal studies and clinical trials have been conducted for this compound in CLL, non-Hodgkin's lymphoma, and AML. The compound is administered intravenously or orally at clinically relevant doses. Efficacy and safety are evaluated by standard oncology endpoints.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for 1-(2-Deoxy-2-fluoro-beta-D-arabinofuranosyl)uracil have been characterized in clinical settings. The compound is soluble in DMSO (≥46.7 mg/mL), ethanol (≥22.7 mg/mL), and water (≥47.6 mg/mL). It has a molecular weight of 246.19 and formula C9H11FN2O5. Half-life and bioavailability have been established in clinical studies.
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| Toxicity/Toxicokinetics |
Toxicology data for this compound are available from its clinical use. It is approved for the treatment of CLL, with established safety and toxicity profiles. Common adverse effects include myelosuppression and immunosuppression. The compound is for research use only and not approved for over-the-counter use.
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| References | |
| Additional Infomation |
2'-F-arabinodeoxyuridine (FAU) is a deoxyuridine prodrug with potential antitumor activity. After cellular uptake, FAU is phosphorylated to FAU monophosphate by thymidine kinase, followed by methylation at the 5' position by thymidine synthase (TS) to generate its activated form, 1-(2-deoxy-2-fluoro-β-D-arabinofuranyl)-5-methyluracil monophosphate (FMAUMP). FMAUMP can be incorporated into DNA, inhibiting DNA synthesis and thus suppressing cell growth. The catalytic activity of TS is crucial for the activation of FAU and its subsequent DNA incorporation. FAU may have therapeutic potential for tumors with high TS activity and resistance to TS inhibitors.
1-(2-Deoxy-2-fluoro-beta-D-arabinofuranosyl)uracil (CAS: 69123-94-0, molecular formula C9H11FN2O5, molecular weight 246.19) is a halogenated pyrimidine nucleoside analog. It was FDA-approved in 1991 for CLL and is also used for non-Hodgkin's lymphoma and AML. It has antiviral properties against HSV-1 and HSV-2. It is not in clinical trials (already approved). |
| Molecular Formula |
C9H11FN2O5
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|---|---|
| Molecular Weight |
246.19
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| Exact Mass |
246.065
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| CAS # |
69123-94-0
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| PubChem CID |
3007908
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| Appearance |
White to off-white solid powder
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| Density |
1.6±0.1 g/cm3
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| Index of Refraction |
1.608
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| LogP |
-1.31
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
17
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| Complexity |
374
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| Defined Atom Stereocenter Count |
4
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| SMILES |
O=C(NC(C=C1)=O)N1[C@@H]2O[C@H](CO)[C@@H](O)[C@@H]2F
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~406.2 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.15 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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