Alovudine
Based on 4 publication(s) in Google Scholar
Alovudine (3'-Fluoro-3'-deoxythymidine) is a mtDNA synthesis inhibitor and a marker of DNA synthesis. Alovudine is less susceptible to inflammatory changes than 18F-Fluorodeoxyglucose (FDG) and thus is a better biomarker in pancreatic cancer. Alovudine shows anti-orthopoxvirus and anti-leukemic activity.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.78%
- CAS 番号: 25526-93-6
- 分子式: C10H13FN2O4
- 分子量:244.22
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Alovudine
MoreDNA/RNA Synthesis アイソフォーム固有の製品をすべて表示
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| ATH-8 cell line | ED50 |
1.4 μM
Compound: 3a
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Protection of ATH8 cells against the cytopathic effect of HIV.
Protection of ATH8 cells against the cytopathic effect of HIV.
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[PMID: 3497272] |
| CCRF-CEM | CC50 |
>100 μM
Compound: 1; FLT
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Cytotoxicity in human CEM/0 cells assessed as reduction in cell viability
Cytotoxicity in human CEM/0 cells assessed as reduction in cell viability
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[PMID: 36099330] |
| CCRF-CEM | CC50 |
0.5 mM
Compound: FLT
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Cytotoxic concentration required to inhibit 50% of HIV-1 in CEM cells
Cytotoxic concentration required to inhibit 50% of HIV-1 in CEM cells
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[PMID: 9341906] |
| CCRF-CEM | EC50 |
>50 μM
Compound: 1, FLT
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Antiretroviral activity against HIV-2 ROD infected in thymidine kinase-deficient human CEM cells assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis
Antiretroviral activity against HIV-2 ROD infected in thymidine kinase-deficient human CEM cells assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis
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[PMID: 24751439] |
| CCRF-CEM | IC50 |
>250 μM
Compound: 1, FLT
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Cytostatic activity against thymidine kinase-deficient human CEM cells assessed as inhibition of cell proliferation after 48 hrs by Coulter counter analysis
Cytostatic activity against thymidine kinase-deficient human CEM cells assessed as inhibition of cell proliferation after 48 hrs by Coulter counter analysis
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[PMID: 24751439] |
| CCRF-CEM | IC50 |
39 μM
Compound: 1, FLT
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Cytostatic activity against human CEM/0 cells expressing thymidine kinase assessed as inhibition of cell proliferation after 48 hrs by Coulter counter analysis
Cytostatic activity against human CEM/0 cells expressing thymidine kinase assessed as inhibition of cell proliferation after 48 hrs by Coulter counter analysis
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[PMID: 24751439] |
| CEM-SS | EC50 |
20 nM
Compound: 1, FLT
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Antiviral activity against HIV-1 subtype 3B infected in CEM-SS cells assessed as inhibition of viral replication after 6 days by XTT assay
Antiviral activity against HIV-1 subtype 3B infected in CEM-SS cells assessed as inhibition of viral replication after 6 days by XTT assay
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[PMID: 22858097] |
| HEL | EC50 |
10 μM
Compound: Alovudine
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Antiviral activity against Human adenovirus 2 infected in HEL cells assessed as inhibition of virus-induced cytopathicity
Antiviral activity against Human adenovirus 2 infected in HEL cells assessed as inhibition of virus-induced cytopathicity
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[PMID: 27742238] |
| HeLa | EC50 |
>400 μM
Compound: 1, FLT, Alovudine
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Cytotoxicity against human HeLa P4/R5 cells after 48 hrs by MTT assay
Cytotoxicity against human HeLa P4/R5 cells after 48 hrs by MTT assay
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[PMID: 22352809] |
| HeLa | EC50 |
0.4 μM
Compound: 1, FLT, Alovudine
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Antiviral activity against HIV1 BaL infected in HeLa P4/R5 cells assessed as reduction of viral infection incubated for 2 hrs followed by incubated in drug-free medium for 46 hrs by single round infection beta-galactosidase reporter gene assay
Antiviral activity against HIV1 BaL infected in HeLa P4/R5 cells assessed as reduction of viral infection incubated for 2 hrs followed by incubated in drug-free medium for 46 hrs by single round infection beta-galactosidase reporter gene assay
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[PMID: 22352809] |
| HeLa | EC50 |
0.8 μM
Compound: 1, FLT, Alovudine
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Antiviral activity against HIV1 3B infected in HeLa P4/R5 cells assessed as reduction of viral infection incubated for 2 hrs followed by incubated in drug-free medium for 46 hrs by single round infection beta-galactosidase reporter gene assay
Antiviral activity against HIV1 3B infected in HeLa P4/R5 cells assessed as reduction of viral infection incubated for 2 hrs followed by incubated in drug-free medium for 46 hrs by single round infection beta-galactosidase reporter gene assay
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[PMID: 22352809] |
| L1210 | IC50 |
0.081 μM
Compound: 1, FLT
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Cytostatic activity against mouse L1210 cells assessed as inhibition of cell proliferation after 48 hrs by Coulter counter analysis
Cytostatic activity against mouse L1210 cells assessed as inhibition of cell proliferation after 48 hrs by Coulter counter analysis
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[PMID: 24751439] |
| MT4 | CC50 |
0.197 μM
Compound: FddThd
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Cytotoxic concentration required to reduce the viability of normal uninfected MT-4 cells by 50%
Cytotoxic concentration required to reduce the viability of normal uninfected MT-4 cells by 50%
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[PMID: 1697345] |
| MT4 | EC50 |
0.001 μM
Compound: FddThd
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Effective concentration achieving 50% protection of MT-4 cells against the cytopathic effect of HIV-1
Effective concentration achieving 50% protection of MT-4 cells against the cytopathic effect of HIV-1
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[PMID: 1697345] |
| MT4 | ED50 |
0.001 μM
Compound: 1
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Concentration required to affect a 50% reduction in the cytopathic effect of HIV for MT-4 cells
Concentration required to affect a 50% reduction in the cytopathic effect of HIV for MT-4 cells
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[PMID: 1527788] |
| MT4 | ED50 |
0.001 μM
Compound: 3d
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Dose required to inhibit cytopathic effect of human immunodeficiency virus replication in MT-4 cells.
Dose required to inhibit cytopathic effect of human immunodeficiency virus replication in MT-4 cells.
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[PMID: 3172142] |
| MT4 | ED50 |
0.001 μM
Compound: FddThd
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Inhibitory activity against HIV-1 replication in MT-4 cells
Inhibitory activity against HIV-1 replication in MT-4 cells
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[PMID: 2754700] |
| T-cell line | ED50 |
0.005 μM
Compound: 1
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Tested for its effective dose required to inhibit the replication of HIV-1 in human T-cell line
Tested for its effective dose required to inhibit the replication of HIV-1 in human T-cell line
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10.1016/S0960-894X(01)81057-X |
Alovudine (5-2000 nM, 6-10 days) depletes mitochondrial DNA, reduces mitochondrial encoded proteins, decreases basal oxygen consumption, decreases cell proliferation and viability, and promotes monocytic differentiationin in AML cells (OCI-AML2 and MV4-11)[3].
Alovudine significantly augmentes DNA damage in BRCA1-/- DT40 cells[4].
Alovudine (0.5-2.5 μM, 6 days) prevents spontaneous cancer cell (MDA-MB-231) metastasis, without significant toxicity[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:OCI-AML2 and MV4-11
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Concentration:500, 2000 nM (OCI-AML2); 50, 200 nM (MV4-11)
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Incubation Time:10 days (OCI-AML2 and MV4-11 cells); 9 days (MV4-11 cells)
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Result:Increased expression of CD11b, a cell surface marker associated with monocytic differentiation.
Induced morphological changes typical of monocytic differentiation.
Alovudine (50-250 μM, 9 days) prevents tumour growth and metastasis in pre-clinical animals implanted into MDA-MB-231 tumour cells[5].
Alovudine (25 mg/kg (a loading dose of 25 mg/kg in 5 minutes), i.v.) reaches the extracellular fluid of the brain not by cerebrospinal fluid, but via the cerebral capillaries in rats[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 25526-93-6
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性状 Solid
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分子量 244.22
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分子式 C10H13FN2O4
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Color White to off-white
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SMILES
OC[C@@H]1[C@@H](F)C[C@H](N2C(NC(C(C)=C2)=O)=O)O1
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別名
3'-Fluoro-3'-deoxythymidine; 3′-Deoxy-3′-fluorothymidine; FLT; 3′-デオキシ-3′-フルオロチミジン
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
High mtDNA content identifies oxidative phosphorylation-driven acute myeloid leukemias and represents a therapeutic vulnerability. [Abstract]2025 Jul 14;10(1):222. PMID: 40653487 -
PLoS Pathog
Anti-orthopoxvirus drugs inhibit lumpy skin disease virus replication by targeting viral DNA polymerase. [Abstract]2026 Jan 26;22(1):e1013903. PMID: 41587213 -
J Med Virol
Drug Repurposing: In Vitro Evaluation of Simeprevir as a Novel Antiviral Drug Against Severe Fever With Thrombocytopenia Syndrome Virus. [Abstract]2025 Oct;97(10):e70655. PMID: 41117261 -
溶剤 & 溶解度
DMSO : 100 mg/mL (409.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 25 mg/mL (102.37 mM)
* "≥" means soluble, but saturation unknown.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (8.52 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (8.52 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
純度とドキュメンテーション
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データシート (281 KB)
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SDS (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Challapalli A, et al. 3'-Deoxy-3'-18F-fluorothymidine positron emission tomography as an early predictor of disease progression in patients with advanced and metastatic pancreatic cancer. Eur J Nucl Med Mol Imaging. 2015 May;42(6):831-40. [Content Brief]
[2]. Smee DF, et al. A review of compounds exhibiting anti-orthopoxvirus activity in animal models. Antiviral Res. 2003 Jan;57(1-2):41-52. [Content Brief]
[3]. Yehudai D, et al. The thymidine dideoxynucleoside analog, alovudine, inhibits the mitochondrial DNA polymerase γ, impairs oxidative phosphorylation and promotes monocytic differentiation in acute myeloid leukemia. Haematologica. 2019 May;104(5):963-972. [Content Brief]
[5]. Mauro-Lizcano M, et al. High mitochondrial DNA content is a key determinant of stemness, proliferation, cell migration, and cancer metastasis in vivo. Cell Death Dis. 2024 Oct 11;15(10):745. [Content Brief]
[6]. Stahle L, et al. Transport of alovudine (3'-fluorothymidine) into the brain and the cerebrospinal fluid of the rat, studied by microdialysis. Life Sci. 2000 Mar 31;66(19):1805-16. [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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 4.0946 mL | 20.4732 mL | 40.9464 mL | 102.3659 mL |
| 5 mM | 0.8189 mL | 4.0946 mL | 8.1893 mL | 20.4732 mL | |
| 10 mM | 0.4095 mL | 2.0473 mL | 4.0946 mL | 10.2366 mL | |
| 15 mM | 0.2730 mL | 1.3649 mL | 2.7298 mL | 6.8244 mL | |
| 20 mM | 0.2047 mL | 1.0237 mL | 2.0473 mL | 5.1183 mL | |
| 25 mM | 0.1638 mL | 0.8189 mL | 1.6379 mL | 4.0946 mL | |
| 30 mM | 0.1365 mL | 0.6824 mL | 1.3649 mL | 3.4122 mL | |
| 40 mM | 0.1024 mL | 0.5118 mL | 1.0237 mL | 2.5591 mL | |
| 50 mM | 0.0819 mL | 0.4095 mL | 0.8189 mL | 2.0473 mL | |
| 60 mM | 0.0682 mL | 0.3412 mL | 0.6824 mL | 1.7061 mL | |
| 80 mM | 0.0512 mL | 0.2559 mL | 0.5118 mL | 1.2796 mL | |
| 100 mM | 0.0409 mL | 0.2047 mL | 0.4095 mL | 1.0237 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Alovudine 関連分類
HY-B1516 関連分類
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