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Other Sizes |
ln Vitro |
Pseudomonas aeruginosa exhibits an 80% reduction in biofilm mass at doses of 0.25–16 μg/mL of nitroline, resulting in a mesh-like structure as opposed to a dense one. Nitroline (2.5–20 μM; 24 hours) efficiently prevents a 4-log decrease in the number of viable cells in small cell lung cancer (SCLC) cells in produced biofilms [1]. and MCL1), as well as increase the phospholipid protein Bim to cause SCLC cells to undergo apoptosis. Research has revealed that nitroxoline alters the expression of MDM2 by causing the destruction of phospholiposomes, which in turn increases the expression of the substrate protein p53 for MDM2 [2].
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ln Vivo |
In the C3H/He bladder subcutaneous model of bladder cancer, nitroxoline (15–60 mg/kg; intragastric gavage) can dramatically decrease tumor growth [3].
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Cell Assay |
Cell Viability Assay[2]
Cell Types: H446, H1882, H1417 and H1688 Cell Tested Concentrations: 2.5 μM, 5 μM, 10 μM, 20 μM Incubation Duration: 24 hrs (hours) Experimental Results: Effectively inhibited the survival of small cell lung cancer (SCLC) cells. Western Blot Analysis[2] Cell Types: H446, H1882, H1417 Cell Tested Concentrations: 5 μM, 10 μM, 20 μM Incubation Duration: 24 hrs (hours) Experimental Results: Anti-apoptotic proteins (such as Bcl-2 and MCL1) are inhibited and pro-apoptotic The protein Bim is upregulated. |
Animal Protocol |
Animal/Disease Models: C3H/He mice were injected with MBT-2 cells [3] into the bladder.
Doses: 15 mg/kg or 60 mg/kg. Route of Administration: po (oral gavage); five times a week, on days 1, 2, 4, and 5. , 7, 8, 10 and 11 days. Experimental Results: Dramatically inhibited tumor growth. |
References |
[1]. A Sobke, et al. The urinary antibiotic 5-nitro-8-hydroxyquinoline (Nitroxoline) reduces the formation and induces the dispersal of Pseudomonas aeruginosa biofilms by chelation of iron and zinc. Antimicrob Agents Chemother. 2012 Nov;56(11):6021-5.
[2]. Jin-Guo Yu, et al. Nitroxoline induces cell apoptosis by inducing MDM2 degradation in small-cell lung cancer. Kaohsiung J Med Sci. 2019 Apr;35(4):202-208. |
Molecular Formula |
C9H6N2O3
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Molecular Weight |
190.1555
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CAS # |
4008-48-4
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Related CAS # |
Nitroxoline-d4
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O([H])C1C([H])=C([H])C(=C2C([H])=C([H])C([H])=NC2=1)[N+](=O)[O-]
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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 |
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 : ~50 mg/mL (~262.94 mM)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 5.2587 mL | 26.2936 mL | 52.5873 mL | |
5 mM | 1.0517 mL | 5.2587 mL | 10.5175 mL | |
10 mM | 0.5259 mL | 2.6294 mL | 5.2587 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.