Nimorazole
Based on 1 publication(s) in Google Scholar
Nimorazole (K-1900), a 2-nitroimidazole, is a hypoxic cell-radiation sensitizer. Nimorazole has anti-infective and anti-protozoal against trichomoniasis. Nimorazole has the potential for head and neck cancer.
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- Pureza: 99.33%
- No. CAS: 6506-37-2
- Fòrmula: C9H14N4O3
- Peso molecular:226.23
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) Nimorazole
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Actividad biológica
Antiparasitic
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
9.8 mM
Compound: 4
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Cytotoxicity against human HCT116 cells incubated for 4 hrs under anaerobic condition measured after 5 days by sulforhodamine B assay
Cytotoxicity against human HCT116 cells incubated for 4 hrs under anaerobic condition measured after 5 days by sulforhodamine B assay
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[PMID: 29253343] |
Nimorazole significantly improves the effect of radiotherapeutic management of supraglottic and pharynx tumors and can be given without major side-effects[1][2].
Nimorazole is the only such agent to have shown a significant effect in a randomized controlled trial in head and neck cancer[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 6506-37-2
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Appearance Solid
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Peso molecular 226.23
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Fòrmula C9H14N4O3
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Color White to light brown
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SMILES
O=[N+](C1=CN=CN1CCN2CCOCC2)[O-]
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Synonyms
K-1900
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Eur J Pharm Biopharm
Bioresorbable, electrospun nonwoven for delayed and prolonged release of temozolomide and nimorazole. [Abstract]2021 Apr:161:29-36. PMID: 33567313
Solvente y solubilidad
DMSO : 125 mg/mL (552.54 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, 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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (9.19 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 (9.19 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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (458 KB)
- English - EN (458 KB)
- Français - FR (458 KB)
- Deutsch - DE (458 KB)
- Norwegian - NO (458 KB)
- Español - ES (458 KB)
- Swedish - SV (458 KB)
- Italian - IT (458 KB)
- Korean - KR (458 KB)
- Portuguese - PT (458 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Peter Wardman, et al. Nitroimidazoles as hypoxic cell radiosensitizers and hypoxia probes: misonidazole, myths and mistakes. Br J Radiol. 2019 Jan;92(1093):20170915. [Content Brief]
[2]. Zohreh Fakhrieh Kashan, et al. Therapeutic effects of Iranian herbal extracts against Trichomonas vaginalis. Iran Biomed J. 2017 Sep;21(5):285-93. [Content Brief]
[3]. Overgaard, J., et al., A randomized double-blind phase III study of nimorazole as a hypoxic radiosensitizer of primary radiotherapy in supraglottic larynx and pharynx carcinoma. Results of the Danish Head and Neck Cancer Study (DAHANCA) Protocol 5-85. Radiother Oncol, 1998. 46(2): p. 135-46. [Content Brief]
[4]. Roy, R.B., S.M. Laird, and L. Heasman, Treatment of trichomoniasis in the female. A comparison of metronidazole and nimorazole. Br J Vener Dis, 1975. 51(4): p. 281-4. [Content Brief]
[5]. Henk, J.M., K. Bishop, and S.F. Shepherd, Treatment of head and neck cancer with CHART and nimorazole: phase II study. Radiother Oncol, 2003. 66(1): p. 65-70. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.4203 mL | 22.1014 mL | 44.2028 mL | 110.5070 mL |
| 5 mM | 0.8841 mL | 4.4203 mL | 8.8406 mL | 22.1014 mL | |
| 10 mM | 0.4420 mL | 2.2101 mL | 4.4203 mL | 11.0507 mL | |
| 15 mM | 0.2947 mL | 1.4734 mL | 2.9469 mL | 7.3671 mL | |
| 20 mM | 0.2210 mL | 1.1051 mL | 2.2101 mL | 5.5254 mL | |
| 25 mM | 0.1768 mL | 0.8841 mL | 1.7681 mL | 4.4203 mL | |
| 30 mM | 0.1473 mL | 0.7367 mL | 1.4734 mL | 3.6836 mL | |
| 40 mM | 0.1105 mL | 0.5525 mL | 1.1051 mL | 2.7627 mL | |
| 50 mM | 0.0884 mL | 0.4420 mL | 0.8841 mL | 2.2101 mL | |
| 60 mM | 0.0737 mL | 0.3684 mL | 0.7367 mL | 1.8418 mL | |
| 80 mM | 0.0553 mL | 0.2763 mL | 0.5525 mL | 1.3813 mL | |
| 100 mM | 0.0442 mL | 0.2210 mL | 0.4420 mL | 1.1051 mL |
Nimorazole Related Classifications
HY-16349 Related Classifications
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