Nitracrine |
Katalog-Nr.GC33400
One-Click Copy Product Info
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Nitracrin hemmt die RNA-Synthese und bindet kovalent, reversibel an DNA, bildet aber auch kovalente Addukte mit DNA in vivo. Nitracrin, ein 1-Nitroacridin-Derivat, ist ein potenter Hypoxie-selektiver Wirkstoff in vitro und ein Antitumor-Medikament. Nitracrin hat gegenÜber den meisten Zellen ZytotoxizitÄt.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 4533-39-5
Sample solution is provided at 25 µL, 10mM.
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Nitracrine is an antitumor drug that has been used clinically for several years.
It is demonstrated during the reduction of ledakrin that a key metabolite, a compound with anadditional five-membered ring attaching to positions 1 and 9 of the acridine core and with the retained 9-aminoalkyl side chain, is formed in all the systems that are studied. It is determined that the reactive nitrogen atoms of this additional ring undergo further transformations resulting in the formation of a six-membered ring produced by the addition of a carbon atom to the dihydropyrazoloacridine ring. Furthermore, it is observed that positions 2 and 4 of ledakrin's acridine ring are susceptible to nucleophilic substitution as revealing by the studies with dithiothreitol. Additionally, although most products from the reduction of ledakrin are extremely unstable, 1-aminoacridinone, producing enzymatically and with dithiothreitol, exhibiting persistent stability under the studied conditions[1].
[1]. Gorlewska K, et al. Products of metabolic activation of the antitumor drug ledakrin (nitracrine) in vitro.
Cell experiment: | Six-week-old male rats are injected with 3-methylcholanthrene (4 mg/animal) for 3 days before decapitation. Livers are removed, homogenized in a homogenizer, and centrifuged for 30 min at 10000g.The activation of ledakrin with the microsomal fraction of rat liver is carried out in 0.16 M Trizma base buffer (pH 7.4). The incubation mixture consists of 125 mM nicotinamide, 100 mM glucose 6-phosphate, 10 mM NADPH, glucose-6-phosphate dehydrogenase (40 units), rat liver microsomes (5 mg/mL), andledakrin (1 mmol)[1]. |
References: [1]. Gorlewska K, et al. Products of metabolic activation of the antitumor drug ledakrin (nitracrine) in vitro. | |
| Cas No. | 4533-39-5 | SDF | |
| Canonical SMILES | O=[N+](C1=CC=CC2=NC3=CC=CC=C3C(NCCCN(C)C)=C21)[O-] | ||
| Formula | C18H20N4O2 | M.Wt | 324.38 |
| Löslichkeit | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.0828 mL | 15.414 mL | 30.828 mL |
| 5 mM | 616.6 μL | 3.0828 mL | 6.1656 mL |
| 10 mM | 308.3 μL | 1.5414 mL | 3.0828 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)