| Size | Price | Stock | Qty |
|---|---|---|---|
| 5g |
|
||
| Other Sizes |
| Targets |
5-Iodouridine targets dihydroorotase, an enzyme involved in pyrimidine biosynthesis, with a Ki of 340 µM for the rat enzyme. As a purine nucleoside analog, it has broad antitumor activity targeting indolent lymphoid malignancies. The compound's mechanism involves incorporation into nucleic acids, leading to disruption of DNA and RNA synthesis. It has shown to enhance the effect of gamma irradiation in hamster cells.
|
|---|---|
| ln Vitro |
5-Iodouridine demonstrates in vitro activity as a nucleoside analog. It inhibits dihydroorotase with a Ki of 340 µM for the rat enzyme. The compound sensitizes Don Chinese hamster lung cells to irradiation in a concentration-dependent manner. It has been used in the synthesis of compounds with antiviral and anticancer activities. The compound's activity is typically assessed in cell viability, proliferation, and radiosensitization assays.
|
| ln Vivo |
In vivo studies for 5-Iodouridine have not been extensively documented in the available literature. As a nucleoside analog, it has potential for in vivo applications in cancer therapy and antiviral treatment. Studies in appropriate animal models would be needed to evaluate its in vivo efficacy, pharmacokinetics, and safety profile. The compound has shown to enhance the effect of gamma irradiation in hamster cells, suggesting potential for use as a radiosensitizer.
|
| Enzyme Assay |
For dihydroorotase inhibition assays, purified rat dihydroorotase is incubated with the substrate and 5-Iodouridine at various concentrations. Enzyme activity is measured spectrophotometrically, and Ki values are calculated from dose-response curves. For radiosensitization studies, cells are treated with the compound and exposed to gamma irradiation, and cell survival is assessed by clonogenic assays. For nucleoside analog activity, cellular assays measuring DNA and RNA synthesis inhibition are used.
|
| Cell Assay |
For cellular studies, appropriate cell lines (e.g., Don Chinese hamster lung cells) are cultured in appropriate media and treated with 5-Iodouridine at various concentrations. Cells are exposed to gamma irradiation, and cell survival is assessed by clonogenic assays to evaluate radiosensitization. Cell viability and proliferation are assessed using MTT or similar assays. DNA and RNA synthesis inhibition is measured by incorporation of radiolabeled precursors. Cytotoxicity is assessed using standard cell viability assays.
|
| Animal Protocol |
For in vivo radiosensitization studies, appropriate animal models of cancer would be used. 5-Iodouridine would be administered via appropriate routes at various doses, followed by tumor irradiation. Tumor growth delay and animal survival would be assessed. Pharmacokinetic parameters including half-life, clearance, and tissue distribution would be determined. However, detailed in vivo protocols for 5-Iodouridine have not been extensively reported in the literature.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of 5-Iodouridine have not been fully characterized in the available literature. The compound has a molecular formula of C9H11IN2O6 and a molecular weight of 370.10. It is a pyrimidine nucleoside with moderate water solubility. As a nucleoside analog, it is expected to be taken up by cells and phosphorylated to the active form. Comprehensive PK studies including bioavailability, half-life, protein binding, and tissue distribution are needed.
|
| Toxicity/Toxicokinetics |
5-Iodouridine is a research compound intended for laboratory use only and is not approved for human therapeutic use. As a halogenated nucleoside analog, it is used in the synthesis of 5-substituted pyrimidine nucleosides with antiviral and anticancer activities. The compound has shown to enhance the effect of gamma irradiation in hamster cells. Standard laboratory safety precautions should be followed when handling this compound.
|
| References | |
| Additional Infomation |
5-Iodouridine is a halogenated nucleoside analog of uridine with molecular formula C9H11IN2O6 and molecular weight 370.10. It inhibits dihydroorotase with a Ki of 340 µM and sensitizes cells to irradiation. The compound is used as a starting material for the synthesis of 5-substituted pyrimidine nucleosides with antiviral and anticancer activities. It is for research use only and has not been approved for clinical applications.
|
| Molecular Formula |
C9H11IN2O6
|
|---|---|
| Molecular Weight |
370.10
|
| Exact Mass |
369.966
|
| CAS # |
1024-99-3
|
| PubChem CID |
1268108
|
| Appearance |
White to off-white solid powder
|
| Density |
2.3±0.1 g/cm3
|
| Melting Point |
205-207ºC (dec.)(lit.)
|
| Index of Refraction |
1.748
|
| LogP |
-0.43
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
18
|
| Complexity |
414
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
C1=C(C(=O)NC(=O)N1[C@H]2[C@@H]([C@@H]([C@H](O2)CO)O)O)I
|
| InChi Key |
RKSLVDIXBGWPIS-UAKXSSHOSA-N
|
| InChi Code |
InChI=1S/C9H11IN2O6/c10-3-1-12(9(17)11-7(3)16)8-6(15)5(14)4(2-13)18-8/h1,4-6,8,13-15H,2H2,(H,11,16,17)/t4-,5-,6-,8-/m1/s1
|
| Chemical Name |
1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-iodopyrimidine-2,4-dione
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : 125 mg/mL (337.75 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.62 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 20.8 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: ≥ 2.08 mg/mL (5.62 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7020 mL | 13.5099 mL | 27.0197 mL | |
| 5 mM | 0.5404 mL | 2.7020 mL | 5.4039 mL | |
| 10 mM | 0.2702 mL | 1.3510 mL | 2.7020 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
