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CAS No.: 144675-97-8

马来酸匹衫琼 Catalog No. CSN12327

Synonyms: BBR 2778;BBR2778 Dimaleate;Pixantrone (maleate)

Pixantrone dimaleate is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity. Pixantrone dimaleate is an experimental antineoplastic drug.

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实验方案

技术信息

生物活性

描述Pixantrone, a Mitoxantrone analogue with low cardiotoxicity, is a topoisomerase II inhibitor, usually used in study of non-Hodgkin's lymphomas as well as an immunosuppressant in multiple sclerosis. Pixantrone may preferentially target on topoisomerase IIα. Incubation with Pixantrone at concentration ranging in 0-100μM (especially 50-100μM) for 1h induced a dose-dependent increase of topoisomerase II-mediated DNA-protein cross-links in HL-60 cells. Pixantrone at concentration of 50μM led to inhibition of topoisomerase II (purified from HL-60 cells)-mediated DNA strand passage. Pixantrone can produce linear double-strand DNA in a pBR322 DNA cleavage assay (10-100μM) and cellular DNA double strand breaks (5-50μM) in K562 cells. Pixantrone can also be used as an immunosuppressive drug. Administration of pixantrone (8, 12, 16.25mg/kg, i.v) reduced the severity of acute and decreased the relapse rate of chronic relapsing EAE rat model, with a marked and long-lasting decrease in CD3+, CD4+, CD8+ and CD45RA+ blood cells and reduced anti-MBP titers observed. Compared with Mitoxantrone, Pixantrone showed much lower cardiotoxicity due to three factors: 1. Its lack of binding to iron(III) makes the inability to induce iron-based oxidative stress; 2. Its lower cellular uptake may limit the production of semiquinone free radicals and redox cycle; 3. Its less potency to topoisomerase IIβ attenuated cardiotoxicity due to topoisomerase IIβ predominates in post-mitotic cardiomyocytes.
动物研究
剂量
CD1 female mice: 27 mg/kg^[2] (i.v.)

给药途径
i.v.
临床研究

动物研究
剂量	CD1 female mice: 27 mg/kg^[2] (i.v.)
给药途径	i.v.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01321541	Diffuse Large B-cell Lymphoma ... more >> de Novo DLBCL DLBCL Transformed From Indolent Lymphoma Follicular Grade 3 Lymphoma Collapse <<	Phase 3	Completed	-	-
NCT00069966	Lymphoma	Phase 2	Unknown	-	-
NCT00551239	Leukemia Lymp... more >>homa Collapse <<	Phase 3	Unknown	-	United States, Washington ... more >> Cell Therapeutics, Incorporated Seattle, Washington, United States, 98119 Collapse <<

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参考文献

[1] Evison BJ, Mansour OC, et al. Pixantrone can be activated by formaldehyde to generate a potent DNA adduct forming agent. Nucleic Acids Res. 2007;35(11):3581-9.
[2] Cavalletti E, Crippa L, et al. Pixantrone (BBR 2778) has reduced cardiotoxic potential in mice pretreated with doxorubicin: comparative studies against doxorubicin and mitoxantrone. Invest New Drugs. 2007 Jun;25(3):187-95.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7937 mL
- 8.9685 mL
- 17.9369 mL
- 5 mM
- 0.3587 mL
- 1.7937 mL
- 3.5874 mL
- 10 mM
- 0.1794 mL
- 0.8968 mL
- 1.7937 mL

技术信息

CAS号

144675-97-8

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H27N5O10

运输

蓝冰

分子量

557.51

别名

BBR 2778;BBR2778 Dimaleate;Pixantrone (maleate);Pixantrone Maleate;马来酸匹衫琼

溶解度

DMSO	98.0 mg/mL (175.8 mM)
Ethanol	1.0 mg/mL (1.8 mM)

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT01321541	Diffuse Large B-cell Lymphoma ... more >> de Novo DLBCL DLBCL Transformed From Indolent Lymphoma Follicular Grade 3 Lymphoma Collapse <<	Phase 3	Completed	-	-
NCT00069966	Lymphoma	Phase 2	Unknown	-	-
NCT00551239	Leukemia Lymp... more >>homa Collapse <<	Phase 3	Unknown	-	United States, Washington ... more >> Cell Therapeutics, Incorporated Seattle, Washington, United States, 98119 Collapse <<
NCT01086605	Breast Cancer	Phase 2	Completed	-	-
NCT01086605	-	-	Completed	-	-
NCT00053105	Lymphoma	Phase 1	Unknown	-	United States, Arizona ... more >> Arizona Clinical Research Center Tucson, Arizona, United States, 85712 United States, Arkansas Highlands Oncology Group Springdale, Arkansas, United States, 72764 United States, California USC/Norris Comprehensive Cancer Center and Hospital Los Angeles, California, United States, 90033-0800 United States, Maryland Marlene and Stewart Greenebaum Cancer Center, University of Maryland Baltimore, Maryland, United States, 21201 United States, Ohio Ireland Cancer Center Cleveland, Ohio, United States, 44106-5055 United States, Tennessee Boston Baskin Cancer Group, University Tennessee Memphis, Tennessee, United States, 38104 United States, Texas University of Texas - MD Anderson Cancer Center Houston, Texas, United States, 77030 Collapse <<

马来酸匹衫琼 Catalog No. CSN12327

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