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Mitoxantrone

产品编号 T6588 CAS 65271-80-9

别名: 米托蒽醌, mitozantrone

Mitoxantrone (mitozantrone) 是一种拓扑异构酶 II 的抑制剂，也可抑制蛋白激酶C (PKC)，IC50值为8.5 μM。

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Mitoxantrone, CAS 65271-80-9

规格	价格/CNY	货期
25 mg	￥ 297	现货
50 mg	￥ 418	现货
100 mg	￥ 617	现货
200 mg	￥ 887	现货
1 mL * 10 mM (in DMSO)	￥ 373	现货

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其他形式的 Mitoxantrone:

Mitoxantrone dihydrochloride
现货
Mitoxantrone diacetate
询价

选择批次

纯度: 98.14%

纯度: 97.97%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Mitoxantrone (mitozantrone) is an anthracenedione antibiotic with antineoplastic activity. Mitoxantrone intercalates into and crosslinks DNA, thereby disrupting DNA and RNA replication. This agent also binds to topoisomerase II, resulting in DNA strand breaks and inhibition of DNA repair. Mitoxantrone is less cardiotoxic compared to doxorubicin.
靶点活性	PKC:8.5 μM.
体外活性	Mitoxantrone induces DNA fragmentation and the proteolytic cleavage of poly(ADP-ribose) polymerase (PARP), a marker of the activation of caspases, in all the patients studied, demonstrating that the cytotoxic effect of mitoxantrone is due to induction of apoptosis. [1] Mitoxantrone activates NFkappaB and stimulates IkappaBalpha degradation in the promyelocytic leukemia cell line HL60 but not in the variant cells, HL60/MX2 cells, which lack the beta isoform of topoisomerase II and express a truncated alpha isoform that results in an altered subcellular distribution. [2] Mitoxantrone inhibits proliferation of activated PBMCs, B lymphocytes, or antigen-specific T-cell lines (TCLs) stimulated on antigen-presenting cells (APCs) in a dose-dependent manner. Mitoxantrone induces apoptosis of PBMCs, monocytes and DCs at low concentrations, whereas higher doses causes cell lysis. [3]
体内活性	Mitoxantrone transiently decreases the growth rate of HID xenografts in mice but does not affect that of PAC120 xenografts. [4] Mitoxantrone results in the severity of the cardiac lesions and the nephropathy and the intestinal toxicity in spontaneously hypertensive rats. Mitoxantrone and iron(III) form a strong 2:1 complex, in which mitoxantrone may be acting as a tridentate ligand. [5]
激酶实验	activity-based protein profiling (ABPP): Mouse brains are Dounce-homogenized in PBS, pH7.5, followed by a low-speed spin (1,400×, 5 min) to remove debris. The supernatant is then subjected to centrifugation (64,000×, 45 min) to provide the cytosolic fraction in the supernatant and the membrane fraction as a pellet. The pellet is washed and resuspended in PBS buffer by sonication. Total protein concentration in each fraction is determined using a protein assay kit. Samples are stored at -80 °C until use. Mouse brain membrane proteomes, are diluted to 1 mg/mL in PBS and pre-incubated with varying concentrations of inhibitors (1 nM to 10 mM) for 30 min at 37 °C before the addition of FP-rhodamine at a final concentration of 2 mM in a 50 mL total reaction volume. After 30 min at 25 °C, the reactions are quenched with 4×SDS-PAGE loading buffer, boiled for 5 min at 90 °C, subjected to SDS-PAGE and visualized in-gel using a flatbed fluorescence s
细胞实验	The human breast carcinoma cell lines MDA-MB-231 and MCF-7 are seeded in standard 96-well plates. One day after seeding, the culture medium is changed and replaced by medium containing different concentration of Mitoxantrone (10-5 to 5 μM) with or without DHA (30 μM) during 7 days. Viability of cells are measured as a whole by the tetrazolium salt assay[3].

别名	米托蒽醌, mitozantrone
分子量	444.48
分子式	C22H28N4O6
CAS No.	65271-80-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 88 mg/mL (197.98 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2498 mL	11.2491 mL	22.4982 mL	56.2455 mL
	5 mM	0.45 mL	2.2498 mL	4.4996 mL	11.2491 mL
	10 mM	0.225 mL	1.1249 mL	2.2498 mL	5.6246 mL
	20 mM	0.1125 mL	0.5625 mL	1.1249 mL	2.8123 mL
	50 mM	0.045 mL	0.225 mL	0.45 mL	1.1249 mL
	100 mM	0.0225 mL	0.1125 mL	0.225 mL	0.5625 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Bellosillo B, et al. Br J Haematol, 1998, 100(1), 142-146. 2. Boland MP, et al. J Biol Chem, 2000, 275(33), 25231-25238. 3. Neuhaus O, et al. J Neuroimmunol, 2005, 168(1-2), 128-137. 4. Oudard S, et al. J Urol, 2003, 169(5), 1729-1734. 5. Herman EH, et al. J Mol Cell Cardiol, 1997, 29(9), 2415-2430. 6. Dong L, Shen S, Chen W, et al. Discovery of Novel Inhibitors Targeting Human O-GlcNAcase: Docking-Based Virtual Screening, Biological Evaluation, Structural Modification, and Molecular Dynamics Simulation[J]. Journal of chemical information and modeling. 2019, 59(10): 4374-4382. 7. Zeng X, Zhu S, Lu W, et al. Target identification among known drugs by deep learning from heterogeneous networks[J]. Chemical Science. 2020, 11(7): 1775-1797.

文献引用

1. Zeng X, Zhu S, Lu W, et al. Target identification among known drugs by deep learning from heterogeneous networks. Chemical Science. 2020, 11(7): 1775-1797. 2. Dong L, Shen S, Chen W, et al. Discovery of Novel Inhibitors Targeting Human O-GlcNAcase: Docking-Based Virtual Screening, Biological Evaluation, Structural Modification, and Molecular Dynamics Simulation. Journal of chemical information and modeling. 2019, 59(10): 4374-4382. 3. Zeng R, Yang X M, Li H W, et al.Simplified Derivatives of Tetrandrine as Potent and Specific P-gp Inhibitors to Reverse Multidrug Resistance in Cancer Chemotherapy.Journal of Medicinal Chemistry.2023 4. Ba D, Li H, Liu R, et al.Exploratory study on the efficacy of bortezomib combining mitoxantrone or CD22-CAR T therapy targeting CD19-negative relapse after CD19-CAR T cell therapy with a simpler cell-line-based model.Apoptosis.2023: 1-12. 5. Yu T, Zeng R, Guan Y, et al.Discovery of new tricyclic spiroindole derivatives as potent P-glycoprotein inhibitors for reversing multidrug resistance enabled by synthetic methodology-based library.RSC Medicinal Chemistry.2024

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Mitoxantrone 65271-80-9 Chromatin/Epigenetic Cytoskeletal Signaling DNA Damage/DNA Repair Topoisomerase PKC leukaemia NSC301739 MCF-7 NSC 301739 lymphocytes HL60 cells NSC-301739 B-CLL cells Protein kinase C inhibit Orthopoxvirus 米托蒽醌 antitumor Endogenous Metabolite Apoptosis breast cancer Inhibitor mitozantrone inhibitor

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Mitoxantrone

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords