Nitracrine
Based on 1 Customer Validation
Nitracrine inhibits RNA synthesis and covalently, reversibly binds to DNA but also forms covalent adducts with DNA in vivo. Nitracrine, a 1-nitroacridine derivative, is a potent hypoxia-selective agent in vitro and antitumor agent. Nitracrine has cytotoxicity towards most cells.
For research use only. We do not sell to patients.
- Purity: 97.04%
- CAS No.: 4533-39-5
- Formula: C18H20N4O2
- Molecular Weight:324.38
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
All DNA/RNA Synthesis Isoforms
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.049 nM
Compound: 4
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Inhibitory activity of compound for AA8 cells to reduce cell density by 50% (exposed to compound for 4 hours)
Inhibitory activity of compound for AA8 cells to reduce cell density by 50% (exposed to compound for 4 hours)
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[PMID: 2909741] |
| CHO-AA8 | IC50 |
0.024 μM
Compound: 2
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Growth inhibitory activity against CHO subline AA8 cells exposed for 18 hr under aerobic conditions
Growth inhibitory activity against CHO subline AA8 cells exposed for 18 hr under aerobic conditions
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[PMID: 1479583] |
| CHO-AA8 | IC50 |
0.024 μM
Compound: 1
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Inhibitory activity against aerobic growth of AA8 cells.
Inhibitory activity against aerobic growth of AA8 cells.
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[PMID: 8691448] |
| CHO-AA8 | IC50 |
26.3 nM
Compound: 4
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Inhibitory activity to reduce cell density by 50% of AA8 cells under aerobic conditions
Inhibitory activity to reduce cell density by 50% of AA8 cells under aerobic conditions
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[PMID: 2909741] |
| CHO-AA8 | IC50 |
26.3 nM
Compound: 2
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Tested for the concentration of the drug to reduce cell numbers to 50 percent of controls against AA8 cells in the microassay
Tested for the concentration of the drug to reduce cell numbers to 50 percent of controls against AA8 cells in the microassay
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[PMID: 2329552] |
| UV4 | IC50 |
0.66 nM
Compound: 4
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Inhibitory concentration required to reduce cell density in UV-4 cells to 50% of controls (cells were exposed to compound for 4 days continuously)
Inhibitory concentration required to reduce cell density in UV-4 cells to 50% of controls (cells were exposed to compound for 4 days continuously)
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[PMID: 2909741] |
| UV4 | IC50 |
2 nM
Compound: 4
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Inhibitory ativity to reduce cell density by 50% of repair deffective mutant UV-4 cells in 96-well cultures under aerobic conditions
Inhibitory ativity to reduce cell density by 50% of repair deffective mutant UV-4 cells in 96-well cultures under aerobic conditions
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[PMID: 2909741] |
Nitracrine (2 μM; 1 hour) causes death of 50% of human erythroleukemia K562 cells under illumination for 48 min. While it is 8.5 hours for Nitracrine on the dark[3].
Nitracrine has LD50s of 0.23 μM, 0.6 μM, 0.16 μM in P388 cell, NIH3T3 cell, and K562 cells under illumination after 1 hour of cells incubation, respectively[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human erythroleukemia K562 cells
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Concentration:2 μM
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Incubation Time:1 hour
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Result:Death of 50% of human erythroleukemia K562 cells were achieved under illumination for 48 min.
Chemical Information
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CAS No. 4533-39-5
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Appearance Solid
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Molecular Weight 324.38
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Formula C18H20N4O2
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Color Brown to reddish brown
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SMILES
O=[N+](C1=CC=CC2=NC3=CC=CC=C3C(NCCCN(C)C)=C21)[O-]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (308.28 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.
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.
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: ≥ 2.5 mg/mL (7.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (7.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Wilson WR, et al. Selective toxicity of nitracrine to hypoxic mammalian cells. Br J Cancer. 1984 Feb;49(2):215-23. [Content Brief]
[2]. Gniazdowski M, et al. Nitracrine and its congeners--an overview. Gen Pharmacol. 1995 May;26(3):473-81. [Content Brief]
[3]. Daghastanli NA, et al. Cytotoxicity of nitroheterocyclic compounds, quinifuryl and nitracrine, towards leukaemic and normal cells on the dark and under illumination with visible light. J Photochem Photobiol B. 2004 Jul 19;75(1-2):27-32. [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, 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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0828 mL | 15.4140 mL | 30.8280 mL | 77.0701 mL |
| 5 mM | 0.6166 mL | 3.0828 mL | 6.1656 mL | 15.4140 mL | |
| 10 mM | 0.3083 mL | 1.5414 mL | 3.0828 mL | 7.7070 mL | |
| 15 mM | 0.2055 mL | 1.0276 mL | 2.0552 mL | 5.1380 mL | |
| 20 mM | 0.1541 mL | 0.7707 mL | 1.5414 mL | 3.8535 mL | |
| 25 mM | 0.1233 mL | 0.6166 mL | 1.2331 mL | 3.0828 mL | |
| 30 mM | 0.1028 mL | 0.5138 mL | 1.0276 mL | 2.5690 mL | |
| 40 mM | 0.0771 mL | 0.3854 mL | 0.7707 mL | 1.9268 mL | |
| 50 mM | 0.0617 mL | 0.3083 mL | 0.6166 mL | 1.5414 mL | |
| 60 mM | 0.0514 mL | 0.2569 mL | 0.5138 mL | 1.2845 mL | |
| 80 mM | 0.0385 mL | 0.1927 mL | 0.3854 mL | 0.9634 mL | |
| 100 mM | 0.0308 mL | 0.1541 mL | 0.3083 mL | 0.7707 mL |