3′-Azido-2′,3′-dideoxyuridine
Based on 1 Customer Validation
3′-Azido-2′,3′-dideoxyuridine (AzdU) is a nucleoside analog of Zidovudine (HY-17413). 3′-Azido-2′,3′-dideoxyuridine is a potent inhibitor of human immunodeficiency virus (HIV) replication in human peripheral blood mononuclear cells (PBMC) with limited toxicity for human bone marrow cells (BMC). 3′-Azido-2′,3′-dideoxyuridine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
For research use only. We do not sell to patients.
- Purity: 99.59%
- CAS No.: 84472-85-5
- Formula: C9H11N5O4
- Molecular Weight:253.21
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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HIV |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CCRF-CEM | IC50 |
2.76 μM
Compound: 2
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Concentration of compound required to inhibit 50% of viral replication of human immunodeficiency virus in CEM-F cells
Concentration of compound required to inhibit 50% of viral replication of human immunodeficiency virus in CEM-F cells
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[PMID: 2754712] |
| CCRF-CEM | IC50 |
69.3 μM
Compound: AZU
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Cytotoxicity against human CEM cells after 5 days
Cytotoxicity against human CEM cells after 5 days
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[PMID: 19948402] |
| MT4 | ED50 |
0.36 μM
Compound: 1d
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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 |
0.43 μM
Compound: AzddUrd
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Effective dose achieving 50% protection of MT-4 cells against the cytopathic effect of HIV
Effective dose achieving 50% protection of MT-4 cells against the cytopathic effect of HIV
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[PMID: 2342078] |
| PBMC | IC50 |
>100 μM
Compound: AZU
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Cytotoxicity against human PBMC after 5 days
Cytotoxicity against human PBMC after 5 days
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[PMID: 19948402] |
| Vero | IC50 |
26 μM
Compound: AZU
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Cytotoxicity against african green monkey Vero cells after 5 days
Cytotoxicity against african green monkey Vero cells after 5 days
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[PMID: 19948402] |
3′-Azido-2′,3′-dideoxyuridine inhibits HIV replication in PBMC infected with HIV-1, with a median effective concentration of 0.18-0.46 μM[2].
3′-Azido-2′,3′-dideoxyuridine inhibits HIV-mediated cytopathic effects in the human T-cell lines MT-4 and ATH8, with the median effective of 0.4 µM[3].
3′-Azido-2′,3′-dideoxyuridine is sequentially phosphorylated to its mono-, di-, and triphosphate metabolites by cellular kinases[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pharmacokinetic Parameters of 3′-Azido-2′,3′-dideoxyuridine in male Sprague-Dawley rats[3].
| IV (25 mg/kg) | IV (100 mg/kg) | PO (25 mg/kg) | PO (100 mg/kg) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Cmax (μg/mL) | 9.2±1.9 | 41±15 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Tmax (h) | 0.38±0.13 | 0.63±0.22 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| AUC (μg/mL∗h) | 19±1.2 | 156±7.0 | 12±0.54 | 70±13 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| CLT (L/h/kg) | 1.4±0.2 | 0.70±0.09 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| CLR (L/h/kg) | 0.90±0.27 | 0.43±0.12 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| t1/2 (h) | 0.5±0.0 | 0.68±0.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
Solvent & SolubilityIn Vitro:
DMSO : 250 mg/mL (987.32 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
View the Complete Stock Solution Preparation Table
Preparing Stock Solutions
View the Complete Stock Solution Preparation Table
Concentration
Solvent
Mass
1 mg
5 mg
10 mg
Concentration
Solvent
Mass
1 mM
3.9493 mL
19.7465 mL
39.4929 mL
5 mM
0.7899 mL
3.9493 mL
7.8986 mL
10 mM
0.3949 mL
1.9746 mL
3.9493 mL
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month. Molarity Calculator
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
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×
×
Dilution Calculator
Concentration (start) × Volume (start) = Concentration (final) × Volume (final) In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route. Stock Solution Working Solution
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline Solubility: ≥ 2.08 mg/mL (8.21 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 (8.21 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. In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Please enter your animal formula composition:
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE). Working solution concentration: 0.22 mg/mL Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact
Method for preparing in vivo working solution for animal experiments:
1. Take μL DMSO stock solution; 2. Add μL . μL , mix evenly; 3. Then add μL Tween 80, mix evenly; 4. Then add μL
Saline
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Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution. 
Purity & Documentation
Select Batch:
Purity:
99.98%
Assay:
99.98%
ee.:
99.98%
References[1]. Zhu Z, et al. Cellular metabolism of 3'-azido-2',3'-dideoxyuridine with formation of 5'-O-diphosphohexose derivatives by previously unrecognized metabolic pathways for 2'-deoxyuridine analogs. Mol Pharmacol. 1990 Dec;38(6):929-38. [Content Brief] [2]. Chu CK, et al. Structure-activity relationships of pyrimidine nucleosides as antiviral agents for human immunodeficiency virus type 1 in peripheral blood mononuclear cells. J Med Chem. 1989 Mar;32(3):612-7. [Content Brief] [3]. Kong L, et al. Pharmacokinetic evaluation of 3'-azido-2', 3'-dideoxyuridine-5'-O-valinate-hydrochloride as a prodrug of the anti-HIV nucleoside 3'-azido-2', 3'-dideoxyuridine. Antivir Chem Chemother. 2003 Sep;14(5):263-70. [Content Brief] 
Complete Stock Solution Preparation TablePlease 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
3′-Azido-2′,3′-dideoxyuridine Related ClassificationsHY-106850 Related ClassificationsKeywords
Assay Types
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