Mitoxantrone HCl
(Synonyms: 米托蒽醌二盐酸盐; Mitozantrone dihydrochloride; NSC 301739 dihydrochloride) 目录号 : GC14363
An inhibitor of DNA topoisomerase IIα and HIV-1 integrase
Cas No.:70476-82-3
Sample solution is provided at 25 µL, 10mM.
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Mitoxantrone is a Topoisomerase II inhibitor, an anti-neoplastic drug for leukemia and other types of cancer, and a proven drug for multiple sclerosis.
Topoisomerase regulates and changes the topologic conditions of DNA during transcription. It plays a role in condensation of chromosome, separation of chromatid and the relief of torsional stress etc.
Mitoxantrone suppressed the leukemia via inhibiting DNA synthesis and cell cycle progression. It had effect on different immune cells (e.g. T cell, B cell and macrophage etc.) [1] It interfered with TOPO-II-mediated DNA cleavage and led to multiple DSB (DNA strand breaks), chromatin structure changes etc. [2] In PDA (pancreatic ductal adenocarcinoma) cell line, mitoxantrone affected cell survival with IC50 < 10 nM and targeted USP11 (human ubiquitin-specific peptidase 11). [3] In human dental pulp stem cells and human dermal fibroblasts, mitoxantrone induced apoptosis or premature senescence in a dose –dependent manner. [4]
In clinical trial, mitoxantrone exhibited a significant but partial efficacy in decreasing the chance of multiple sclerosis progression and relapses frequency in patient with worsening RRMS, PRMS and SPMS in a 2 years follow-up study. [5]
References:
[1] Fox EJ. Mechanism of action of mitoxantrone. Neurology. 2004 Dec 28;63(12 Suppl 6):S15-8.
[2] Awasthi P, Dogra S, Barthwal R. Multispectroscopic methods reveal different modes of interaction of anticancer drug mitoxantrone with Poly(dG-dC).Poly(dG-dC) and Poly(dA-dT).Poly(dA-dT). J Photochem Photobiol B. 2013 Oct 5;127:78-87.
[3] Burkhart RA, Peng Y, Norris ZA et al. Mitoxantrone targets human ubiquitin-specific peptidase 11 (USP11) and is a potent inhibitor of pancreatic cancer cell survival. Mol Cancer Res. 2013 Aug;11(8):901-11.
[4] Seifrtova M, Havelek R, Soukup T, Filipova A, Mokry J, Rezacova M. Mitoxantrone ability to induce premature senescence in human dental pulp stem cells and human dermal fibroblasts. J Physiol Pharmacol. 2013 Apr;64(2):255-66.
[5] Martinelli Boneschi F, Vacchi L, Rovaris M, Capra R, Comi G. Mitoxantrone for multiple sclerosis. Cochrane Database Syst Rev. 2013 May 31;5:CD002127.
| Cell experiment [1]: | |
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Cell lines |
DPSCs and HDFs |
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Preparation method |
The solubility of this compound in DMSO is > 18.2 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
5, 20, 50, 100 and 150 nM |
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Applications |
Mitoxantrone HCl almost completely inhibited DPSCs and HDFs proliferation without causing significant decrease in cell viability after 6 days. Mitoxantrone HCl, at higher doses, i.e. 100 nM and 150 nM, significantly decreased DPSCs and HDFs viability after 3 days. In addition, Mitoxantrone HCl at doses over 50 nM significantly increased the activity of caspases 3/7 and the level of puma, inducing DPSCs and HDFs apoptosis. |
| Animal experiment [2]: | |
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Animal models |
Mice bearing PAC120 and HID xenografts |
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Dosage form |
1 mg/kg; i.p.; once per 3 weeks |
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Applications |
In mice bearing PAC120 xenografts, Mitoxantrone HCl was well tolerated, although it caused a weight loss of 10% or less. However, it did not inhibit tumor growth. In mice bearing HID xenografts, Mitoxantrone HCl transiently inhibited tumor growth with the optimal effect 3 weeks after the start of treatment. After 30 days, Mitoxantrone HCl no longer exhibited any inhibitory effect on tumor growth. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Seifrtova M, Havelek R, Soukup T, Filipova A, Mokry J, Rezacova M. Mitoxantrone ability to induce premature senescence in human dental pulp stem cells and human dermal fibroblasts. J Physiol Pharmacol. 2013 Apr;64(2):255-66. [2]. Oudard S, Legrier ME, Boyé K, Bras-Gonalves R, De Pinieux G, De Cremoux P, Poupon MF. Activity of docetaxel with or without estramustine phosphate versus mitoxantrone in androgen dependent and independent human prostate cancer xenografts. J Urol. 2003 May;169(5):1729-34. | |
| Cas No. | 70476-82-3 | SDF | |
| 别名 | 米托蒽醌二盐酸盐; Mitozantrone dihydrochloride; NSC 301739 dihydrochloride | ||
| 化学名 | 1,4-dihydroxy-5,8-bis[2-(2-hydroxyethylamino)ethylamino]anthracene-9,10-dione;dihydrochloride | ||
| Canonical SMILES | C1=CC(=C2C(=C1NCCNCCO)C(=O)C3=C(C=CC(=C3C2=O)O)O)NCCNCCO.Cl.Cl | ||
| 分子式 | C22H29ClN4O6.HCl | 分子量 | 517.4 |
| 溶解度 | ≥ 18.2mg/mL in DMSO | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9327 mL | 9.6637 mL | 19.3274 mL |
| 5 mM | 0.3865 mL | 1.9327 mL | 3.8655 mL |
| 10 mM | 0.1933 mL | 0.9664 mL | 1.9327 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet