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Luotonin A

Catalog No.GC15612

binds to and stabilizes the topoisomerase I-DNA binary complex

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Luotonin A Chemical Structure

Cas No.: 205989-12-4

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1mg
44,00 $US
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5mg
97,00 $US
En stock
10mg
131,00 $US
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Sample solution is provided at 25 µL, 10mM.

Description of Luotonin A

IC50: 1.8 μg/mL for P-388 cell line

Luotonin A binds to and stabilizes the topoisomerase I-DNA binary complex.

Topoisomerase DNA complexes have been reported as the primary target of several important antitumor agents. These agents have been shown to be able to increase the number of topoisomerase-associated DNA strand breaks in cells, by stabilizing the covalent enzyme-DNA complex and therefore diminishing the resealing of the DNA phosphodiester linkages

In vitro: Luotonin A was isolated as a pyrroloquinazolinoquinoline alkaloid from the Chinese medicinal plant Peganum nigellastrum. Luotonin A could stabilize the human DNA topoisomerase I-DNA covalent binary complex and mediate topoisomerase I-dependent cytotoxicity in intact cells. Similar to camptothecin, luotonin A was able to effect concentration-dependent stabilization of the enzyme-DNA binary complex. However, neither camptothecin nor luotonin A had any measurable effect on DNA in the absence of topoisomerase I. In addition, luotonin A was evaluated in a strain of Saccharomyces cereVisiae lacking yeast topoisomerase I, but having a plasmid having the human topoisomerase I gene under the control of a galactose promoter. Results showed that luotonin A at 1 μM concentration could produce 36% inhibition of growth in the presence of galactose. Moreover, in replicate experiments, lutonin A exhibited IC50 values from 5.7 to 12.6 μM in the presence of galactose, while the comparable values for camptothecin were from 0.74 to 0.86 μM [1].

In vivo: Up to now, there is no animal in vivo data reported.

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Cagir, A. ,Jones, S.H.,Gao, R., et al. Luotonin A. A naturally occurring human DNA topoisomerase I poison. Journal of the American Chemical Society 125(45), 13628-13629 (2003).

Chemical Properties of Luotonin A

Cas No. 205989-12-4 SDF
Chemical Name quino[2',3':3,4]pyrrolo[2,1-b]quinazolin-11(13H)-one
Canonical SMILES O=C1N2C(C(N=C(C=CC=C3)C3=C4)=C4C2)=NC5=CC=CC=C51
Formula C18H11N3O M.Wt 285.3
Solubility ≤3mg/ml in DMSO;3mg/ml in dimethyl formamide 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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Luotonin A

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1 mg 5 mg 10 mg
1 mM 3.5051 mL 17.5254 mL 35.0508 mL
5 mM 0.701 mL 3.5051 mL 7.0102 mL
10 mM 0.3505 mL 1.7525 mL 3.5051 mL
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In vivo Formulation Calculator (Clear solution) of Luotonin A

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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 ddH2O, 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.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 1 reference(s) in Google Scholar.)

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