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Pixantrone

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Chemical Structure| 144675-97-8 同义名 : 匹克生琼来酸盐 ;Pixantrone (maleate);Pixantrone Maleate;BBR 2778
CAS号 : 144675-97-8
货号 : A387062
分子式 : C25H27N5O10
纯度 : 99%+
分子量 : 557.509
MDL号 : MFCD00920108
存储条件:

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(89.68 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 8 mg/mL(14.35 mM),配合低频超声,并水浴加热至45℃助溶

动物实验配方:
生物活性
描述 Pixantrone dimaleate induces cell death in various cancer cell lines regardless of cell cycle perturbation, with IC50 values of 37.3 nM, 126 nM, and 136 nM for T47D, MCF-10A, and OVCAR5 cells, respectively, after treatment with concentrations ranging from 0 to 10 μM for 72 hours [1]. Pixantrone dimaleate induces DNA damage at a high concentration of 500 nM after treatment for 24 hours, leading to severe chromosomal aberrations and mitotic catastrophe in PANC1 cells [1]. Pixantrone dimaleate at a concentration of 100 nM for 24 hours may interfere with chromosome segregation by generating merotelic kinetochore attachments, leading to chromosome non-disjunction [1]. Pixantrone dimaleate exhibits potent growth inhibition of human leukemia K562 cells, etoposide-resistant K/VP.5 cells, MDCK, and ABCB1-transfected MDCK/MDR cells, with IC50 values of 0.10 μM, 0.56 μM, 0.058 μM, and 4.5 μM, respectively, after treatment with concentrations ranging from 0 to 100 μM for 72 hours [2]. Pixantrone dimaleate (0.01-0.2 μM) induces the concentration-dependent formation of linear DNA by targeting topoisomerase IIα and generates semiquinone free radicals in an enzymatic reducing system, although not in a cellular system, possibly due to low cellular uptake [2]. Pixantrone dimaleate (0.01-10 μM) exhibits strong inhibitory effects on rat 97-116 peptide-specific T cell proliferation [4].
临床研究
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 ... 展开 >> de Novo DLBCL DLBCL Transformed From Indolent Lymphoma Follicular Grade 3 Lymphoma 收起 << Phase 3 Completed - -
NCT00069966 Lymphoma Phase 2 Unknown - -
NCT00551239 Leukemia Lymp... 展开 >>homa 收起 << Phase 3 Unknown - United States, Washington ... 展开 >> Cell Therapeutics, Incorporated Seattle, Washington, United States, 98119 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.79mL

0.36mL

0.18mL

8.97mL

1.79mL

0.90mL

17.94mL

3.59mL

1.79mL

参考文献

[1]Beeharry N, et al. Pixantrone induces cell death through mitotic perturbations and subsequent aberrant cell divisions. Cancer Biol Ther. 2015;16(9):1397-406.

[2]Hasinoff BB, et al. Mechanisms of Action and Reduced Cardiotoxicity of Pixantrone; a Topoisomerase II Targeting Agent with Cellular Selectivity for the Topoisomerase IIα Isoform. J Pharmacol Exp Ther. 2016 Feb;356(2):397-409.

[3]Cavalletti E, 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.

[4]Ubiali F, et al. Pixantrone (BBR2778) reduces the severity of experimental autoimmune myasthenia gravis in Lewis rats. J Immunol. 2008 Feb 15;180(4):2696-703.