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/ 拓扑异构酶 / Mitoxantrone/米托蒽醌

Mitoxantrone/米托蒽醌 {[allProObj[0].p_purity_real_show]}

货号：A207951 同义名： Mitozantrone; NSC 301739

Mitoxantrone是一种拓扑异构酶II抑制剂，具有抗肿瘤活性，同时可抑制蛋白激酶C，适用于B-CLL细胞凋亡研究。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Mitoxantrone/米托蒽醌 化学结构 CAS号：65271-80-9
Mitoxantrone/米托蒽醌 化学结构
CAS号：65271-80-9
Mitoxantrone/米托蒽醌 3D分子结构
CAS号：65271-80-9
Mitoxantrone/米托蒽醌 化学结构 CAS号：65271-80-9
Mitoxantrone/米托蒽醌 3D分子结构 CAS号：65271-80-9
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Mitoxantrone/米托蒽醌 纯度/质量文件 产品仅供科研

货号：A207951 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Topo I ↓ Topo II ↓ Topo IV ↓ Topoisomerase ↓ 其他靶点 纯度
Ellagic acid ✔ 98%
β-Lapachone ✔ 99%+
(s)-10-hydroxycamptothecin ✔ 98+%
Camptothecin ++

Topo I, IC50: 0.68 μM

 		98%
Betulinic acid ++

Eukaryotic topoisomerase I, IC50: 5 μM

 		98%
Topotecan ++++

Topo I (MCF-7 Luc cells), IC50: 13 nM

Topo I (DU-145 Luc cells), IC50: 2 nM

 		98%
Irinotecan HCl Trihydrate ✔ 98%
SN-38 ✔ 98%
Levofloxacin hydrate ✔ 98%
Dexrazoxane ✔ 99%+
Ofloxacin ✔ 98+%
Enoxacin ✔ 99%+
Flumequine +

Topo II, IC50: 15 μM

 		98%
Levofloxacin ✔ 97%
Etoposide ✔ 98%
Pefloxacin mesylate dihydrate ✔ 99.5%
Marbofloxacin ✔ 98+%
Voreloxin HCl ✔ 98%
Mitoxantrone 2HCl ✔ PKC 98%
Nalidixic acid ✔ 98%
Doxorubicin ✔ 97%
Novobiocin sodium ✔ 95%
Amonafide ✔ 99%+
Pirarubicin ✔ 98%+
Idarubicin HCl +++

Topo II (MCF-7 cells), IC50: 3.3 ng/mL

 		99%+
Genistein ✔ EGFR 98%
Teniposide ✔ 98%
Moxifloxacin ✔ 98%
Ciprofloxacin ✔ 98%
Clinafloxacin ✔ 99%
Gatifloxacin ✔ 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

 		98%
Epirubicin HCl ✔ 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Mitoxantrone/米托蒽醌 生物活性

描述 Mitoxantrone functions as a potent inhibitor of topoisomerase II and also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. It induces apoptosis in B-CLL (B-chronic lymphocytic leukemia) cells and exhibits antitumor activity[1][2][3][4]. Mitoxantrone additionally demonstrates anti-orthopoxvirus activity, with EC50 values of 0.25 μM for cowpox and 0.8 μM for monkeypox, respectively[5].
体内研究

Mitoxantrone administration (IP, 0-3.2 mg/kg/day) leads to a statistically significant increase in the number of 60-day survivors in mice implanted with IP L1210 leukemia, particularly at the dose of 1.6 mg/kg[4].

Mitoxantrone administration (IV, 0-3.2 mg/kg/day) demonstrates potent antitumor effects, resulting in a 60% increase in lifespan (ILS) at a dose of 3.2 mg/kg in mice with subcutaneously implanted Lewis lung carcinoma[4].
体外研究

Mitoxantrone competitively inhibits PKC in relation to histone H1, with a Ki value of 6.3 μM, and non-competitively inhibits PKC with respect to phosphatidylserine and ATP[1].

Mitoxantrone treatment (0.5 μg/mL, 48 h) results in reduced B-CLL cell viability. This effect is accompanied by DNA fragmentation and proteolytic cleavage of poly(ADP-ribose) polymerase (PARP), indicating Mitoxantrone's cytotoxicity is mediated through apoptosis induction[2].

Mitoxantrone exhibits cytotoxic effects on human breast carcinoma cell lines MDA-MB-231 and MCF-7, with IC50 values of 18 and 196 nM, respectively[3].

Mitoxantrone/米托蒽醌 动物研究

Dose Rabbit: 0.5 mg/kg - 2 mg/kg[3] (i.p.) Rat: 2.5 mg/kg[4] (i.p./i.v.) Mice: 0.4 mg/kg - 3.2 mg/kg[5] (i.p.)
Administration i.p., i.v.

Mitoxantrone/米托蒽醌 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
NCT01142466 Multiple Sclerosis, Relapsing-... 展开 >>Remitting 收起 << Phase 4 Completed - -
NCT01142466 - Completed - -
NCT01055483 Acute Myeloid Leukemia Phase 1 Completed - France ... 展开 >> Novartis Investigative Site Paris Cedex 4, France, 75181 Novartis Investigative Site Paris, France, 75475 Germany Novartis Investigative Site Dresden, Germany, 01307 Novartis Investigative Site Frankfurt, Germany, 60590 Novartis Investigative Site Hannover, Germany, 30625 Novartis Investigative Site Ulm, Germany, 89081 收起 <<

Mitoxantrone/米托蒽醌 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.

[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.

[3]Vibet S, et al. Differential subcellular distribution of mitoxantrone in relation to chemosensitization in two human breast cancer cell lines. Drug Metab Dispos. 2007 May;35(5):822-8.

[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.

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

Mitoxantrone/米托蒽醌 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.25mL

0.45mL

0.22mL

11.25mL

2.25mL

1.12mL

22.50mL

4.50mL

2.25mL

Mitoxantrone/米托蒽醌 技术信息

CAS号65271-80-9
分子式C22H28N4O6
分子量 444.48
SMILES Code O=C1C2=C(C(NCCNCCO)=CC=C2NCCNCCO)C(C3=C(O)C=CC(O)=C13)=O
MDL No. MFCD00242942
别名 Mitozantrone; NSC 301739
运输蓝冰
InChI Key KKZJGLLVHKMTCM-UHFFFAOYSA-N
Pubchem ID 4212
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, sealed in dry, 2-8°C
溶解方案

DMSO: 60 mg/mL(134.99 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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案一
方案二

Tags: Mitoxantrone | Mitozantrone;NSC 301739 | Topoisomerase | AmBeed-信号通路专用抑制剂 | Mitoxantrone/米托蒽醌 纯度/质量文件 | Mitoxantrone/米托蒽醌 亚型比较 | Mitoxantrone/米托蒽醌 生物活性 | Mitoxantrone/米托蒽醌 动物研究 | Mitoxantrone/米托蒽醌 临床数据 | Mitoxantrone/米托蒽醌 参考文献 | Mitoxantrone/米托蒽醌 实验方案 | Mitoxantrone/米托蒽醌 技术信息

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