Mitoxantrone HCl.|70476-82-3|(盐酸米托蒽醌; Mitozantrone dihydrochloride; NSC 301739 dihydrochloride)-陌孚医药/Medlife

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Mitoxantrone HCl. (Synonyms: 盐酸米托蒽醌; Mitozantrone dihydrochloride; NSC 301739 dihydrochloride)

目录号: PC16700 纯度: ≥98%

CAS No. :70476-82-3

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中文名称	Mitoxantrone HCl.
中文别名	盐酸米托蒽醌;1,4-二羟基-5,8-双[[2-[(2-羟基乙基)氨基]乙基]氨基]-9,10-蒽醌二盐酸盐;盐酸米托蒽醌 EP标准品;盐酸米托蒽醌 Mitoxantrone HCl;盐酸米托蒽醌 USP标准品;盐酸米托蒽醌标准品;盐酸米托蒽醌（暂行）;(-)-石杉碱甲;1,4-二羟基-5,8-双[[2-[(2-羟乙基)氨基]乙基]氨基]-9,10-蒽醌二盐酸盐;米托蒽醌二盐酸盐;米托蒽醌盐酸盐;1,4-二羟基-5,8-双[[2-[(2-羟乙基)氨基]乙基]氨基]蒽-9,10-二酮二盐酸盐盐酸米托蒽醌;1,4-二羟基-5,8-双[[2-[(2-羟乙基)氨基]乙基]氨基]蒽醌二盐酸盐盐酸米托蒽醌
英文名称	Mitoxantrone HCl
英文别名	Mitoxantrone hydrochloride;1,4-Dihydroxy-5,8-bis[[2-[(2-hydroxyethyl)amino]ethyl]amino]anthraquinone dihydrochloride;Mitozantrone hydrochloride;Novantrone;Mitoxantrone dihydrochloride;1,4-dihydroxy-5,8-bis[2-(2-hydroxyethylamino)ethylamino]anthracene-9,10-dione,dihydrochloride;Mitoxantron HCl;Mitoxantrone (hydrochloride);Mitoxantrone Dihydro;Mitoxantrone HCl;mitozantrone dihydrochloride;1,4-Dihydroxy-5,8-bis-[2-(2-hydroxyethylamino)ethylamino]anthraquinone dihydrochloride;1,4-Dihydroxy-5,8-bis[[2-[(2-hydroxyethyl)amino]ethyl]amino]-9,10-anthracenedione dihydrochloride;1,4-Dihydroxy-5,8-bis[[2-[(2-hydroxyethyl)amino]ethyl]amino]anthracene-9,10-dione Dihydrochloride;Novantron;Immunex;Mitoxantrone 2HCl;Bisantrone;DHAD;Mitoxantrone (dihydrochloride);MITOXANTHRONE HYDROCHLORIDE;U6USW86RD0;1,4-dihydroxy-5,8-bis-[2-(2-hydroxyethylamino)ethylamino]anthraquinone 2hcl;CL 232315;novatrone;1,4-Dihydroxy-5,8-bis((2-((2-hydroxyethyl)amino)e
Cas No.	70476-82-3
分子式	C₂₂H₃₀Cl₂N₄O₆
分子量	517.40
包装储存	4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

生物活性

Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC₅₀ of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity. Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC₅₀s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively.

性状

Solid

IC50 & Target[1][2]

PKC

8.5 μM (IC₅₀)

Topoisomerase II

体外研究(In Vitro)

Mitoxantrone dihydrochloride inhibits PKC in a competitive manner with respect to histone H1, and its K_i value is 6.3 μM and in a non-competitive manner with respect to phosphatidylserine and ATP.
Mitoxantrone dihydrochloride (0.5 μg/mL, 48 h) induces a decrease in B-CLL cells. Mitoxantrone dihydrochloride induces DNA fragmentation and the proteolytic cleavage of poly(ADP-ribose) polymerase (PARP), demonstrating that the cytotoxic effect of Mitoxantrone dihydrochloride is due to induction of apoptosis.
Mitoxantrone dihydrochloride shows cytotoxicity to human breast carcinoma cell lines MDA-MB-231 and MCF-7 with IC₅₀ values of 18 and 196 nM, respectively.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Mitoxantrone dihydrochloride (IP, 0-3.2 mg/kg/day) produces a statistically significant number of 60-day survivors at 1.6 mg/kg in mice with IP implanted L1210 leukemia.
Mitoxantrone dihydrochloride (IV, 0-3.2 mg/kg/day) shows effective antitumor activities and produces a 60% ILS (increase in lifespan) at 3.2 mg/kg in SC implanted Lewis lung carcinoma.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

ClinicalTrial

参考文献

[1]. Takeuchi N, et al. Inhibitory effect of mitoxantrone on activity of protein kinase C and growth of HL60 cells. J Biochem. 1992 Dec;112(6):762-7. [Information]

[2]. Bellosillo B, et al. Mitoxantrone, a topoisomerase II inhibitor, induces apoptosis of B-chronic lymphocytic leukaemia cells. Br J Haematol. 1998 Jan;100(1):142-6. [Information]

[3]. Venza I, et al. Class II-specific histone deacetylase inhibitors MC1568 and MC1575 suppress IL-8 expression in human melanoma cells. Pigment Cell Melanoma Res. 2013 Mar;26(2):193-204. [Information]

[4]. Fujimoto S, et al. Antitumor activity of mitoxantrone against murine experimental tumors: comparative analysis against various antitumor antibiotics. Cancer Chemother Pharmacol. 1982;8(2):157-62. [Information]

[5]. Sharon E Altmann, et al. Inhibition of cowpox virus and monkeypox virus infection by mitoxantrone. Antiviral Res. 2012 Feb;93(2):305-308. [Information]

溶解度数据

体外研究:

H₂O : 100 mg/mL (193.27 mM; Need ultrasonic)

DMSO : ≥ 43 mg/mL (83.11 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.83 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.83 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.83 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.83 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： PBS
Solubility: 2 mg/mL (3.87 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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