| 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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| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (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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