| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Cytidine triphosphate synthase[1]
The primary target of 3-Deazauridine is CTP synthetase, an enzyme that catalyzes the conversion of UTP to CTP, a critical step in pyrimidine nucleotide biosynthesis. By inhibiting CTP synthetase, 3-Deazauridine depletes intracellular CTP pools, leading to reduced DNA and RNA synthesis and inhibition of cell proliferation. The compound is a pyrimidine nucleoside analogue that is incorporated into RNA, further contributing to its anticancer effects. |
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| ln Vitro |
3-Deazauridine (DAUR) has superior anti-tumor properties when applied to L1210 leukemia cells [1].
In vitro, 3-Deazauridine demonstrates anticancer activity against various cancer cell lines. As a pyrimidine nucleoside analogue, it inhibits CTP synthetase, depleting CTP pools and inhibiting DNA and RNA synthesis. The compound has been studied for its activity against leukemia and solid tumor cell lines. The exact IC₅₀ values vary depending on the cell line and are not consistently reported in the available literature. 3-Deazauridine is also known as NSC 126849. |
| ln Vivo |
3-Deazauridine (DAUR) (250 mg/kg/day; intraperitoneally; days 1–9) inhibits L1210 leukemia cells in mice with modest efficacy [1]. 3-Deazauridine (intraperitoneal injection; 5 doses): In beagle dogs and rhesus monkeys, the lethal doses are 250 mg/kg/day and 417 mg/kg/day, respectively; the lowest toxic doses are 62.5 mg/kg/day and 104 mg/kg/day, while the non-toxic doses are 31.25 mg/kg/day and 52 mg/kg/day, respectively[1].
In vivo, 3-Deazauridine has been studied in animal models of cancer. As a CTP synthetase inhibitor, it depletes CTP pools and inhibits tumor growth. The compound has been evaluated in preclinical studies for the treatment of leukemia and other cancers. However, detailed in vivo efficacy data, including tumor growth inhibition and survival rates, are limited in the available literature. The compound's clinical development has been explored in combination with other chemotherapeutic agents. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for 3-Deazauridine typically involve CTP synthetase inhibition studies. The enzyme is incubated with varying concentrations of 3-Deazauridine (0.1-100 µM) in appropriate buffer. CTP synthetase activity is measured by monitoring the conversion of UTP to CTP using radioisotopic or spectrophotometric methods. The IC₅₀ value is calculated from the dose-response curve. The compound demonstrates concentration-dependent inhibition of CTP synthetase activity.
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| Cell Assay |
In vitro cellular assays for 3-Deazauridine involve testing its anticancer activity against various cancer cell lines. Cells are treated with serial dilutions of 3-Deazauridine (0.01-100 µM) for 48-72 hours. Cell viability is assessed using MTT or CCK-8 assays. Apoptosis is measured by Annexin V/PI staining and caspase activity assays. CTP levels in treated cells are measured by HPLC or mass spectrometry to confirm target engagement. The compound demonstrates concentration-dependent anticancer activity.
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| Animal Protocol |
In vivo animal studies for 3-Deazauridine involve efficacy testing in tumor-bearing models. Mice implanted with cancer cells are treated with 3-Deazauridine via intraperitoneal or intravenous administration at various doses. Tumor volume and body weight are monitored over 2-4 weeks. CTP levels in tumors are assessed to confirm target engagement. The compound demonstrates antitumor activity in preclinical models.
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| ADME/Pharmacokinetics |
3-Deazauridine has a molecular formula of C₉H₁₁N₃O₅ and a molecular weight of 241.20. The compound is a pyrimidine nucleoside analogue with anticancer activity. It is intended for research use only and has not been approved for clinical use. Detailed pharmacokinetic parameters such as half-life, oral bioavailability, and tissue distribution are not well characterized in the available literature. The compound is typically stored under recommended conditions.
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| Toxicity/Toxicokinetics |
The toxicity profile of 3-Deazauridine has been characterized in preclinical studies. As a nucleoside analogue, it may have myelosuppressive and gastrointestinal side effects similar to other antimetabolites. Standard toxicity studies include assessment of body weight changes, hematological parameters, and histopathological examination of major organs in animal models. The compound is intended for research use only and is not approved for clinical use.
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| References | |
| Additional Infomation |
3-Denitrouridine is an N-glycoside compound. It is a synthetic analog of the nucleoside uridine, lacking a cyclic nitrogen atom at the 3-position. 3-Denitrouridine inhibits cytidine synthase, thereby reducing intracellular levels of cytidine and deoxycytidine, and interfering with DNA and RNA synthesis. This drug may induce apoptosis and promote tumor cell differentiation. (NCI04) 4-Hydroxy-1-(β-D-ribofuranosyl)-2-pyridone. A uridine analog lacking a cyclic nitrogen atom at the 3-position. It possesses antitumor activity.
3-Deazauridine (CAS 23205-42-7) is a pyrimidine nucleoside analogue with anticancer activity. It has a molecular formula of C₉H₁₁N₃O₅ and a molecular weight of 241.20. The compound inhibits CTP synthetase, depleting CTP pools and inhibiting DNA and RNA synthesis. It has been studied for the treatment of leukemia and solid tumors. 3-Deazauridine is intended for research use only and is not approved for clinical use. |
| Molecular Formula |
C10H13NO6
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|---|---|
| Molecular Weight |
243.21
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| Exact Mass |
243.074
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| CAS # |
23205-42-7
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| PubChem CID |
54684286
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.718g/cm3
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| Boiling Point |
528ºC at 760mmHg
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| Melting Point |
233-235ºC
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| Flash Point |
273.1ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.706
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| LogP |
-1.8
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| Hydrogen Bond Donor Count |
4
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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 |
379
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C1=CN(C(=O)C=C1O)[C@H]2[C@@H]([C@@H]([C@H](O2)CO)O)O
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| InChi Key |
CBOKZNLSFMZJJA-PEBGCTIMSA-N
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| InChi Code |
InChI=1S/C10H13NO6/c12-4-6-8(15)9(16)10(17-6)11-2-1-5(13)3-7(11)14/h1-3,6,8-10,12-13,15-16H,4H2/t6-,8-,9-,10-/m1/s1
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| Chemical Name |
1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-4-hydroxypyridin-2-one
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (411.17 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (8.22 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 20.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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 mg/mL (8.22 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1117 mL | 20.5584 mL | 41.1167 mL | |
| 5 mM | 0.8223 mL | 4.1117 mL | 8.2233 mL | |
| 10 mM | 0.4112 mL | 2.0558 mL | 4.1117 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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