Luotonin A

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Luotonin A

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

205989-12-4

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议

产品介绍

化学性质

Physical Appearance	A crystalline solid
Storage	Store at -20°C
M.Wt	285.3
Cas No.	205989-12-4
Formula	C₁₈H₁₁N₃O
Solubility	≤3mg/ml in DMSO;3mg/ml in dimethyl formamide
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
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

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).