Mitoxantrone dihydrochloride 是一种有效的拓扑异构酶II (topoisomerase II) 抑制剂。Mitoxantrone dihydrochloride 也可抑制蛋白激酶 C (PKC)，其IC50值为 8.5 μM。Mitoxantrone dihydrochloride 诱导 B- 慢性淋巴细胞白血病 (B-CLL) 细胞凋亡 (apoptosis)。Mitoxantrone dihydrochloride 具有抗肿瘤活性。Mitoxantrone dihydrochloride 还具有抗正痘病毒 (orthopoxvirus) 活性，对牛痘和猴痘的EC50分别为 0.25 μM 和 0.8 μM。
| 生物活性 | Mitoxantrone dihydrochloride is a potenttopoisomeraseIIinhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with anIC50of 8.5 μM. Mitoxantrone dihydrochloride inducesapoptosisof B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity[1][2][3][4]. Mitoxantrone dihydrochloride also has anti-orthopoxvirusactivity withEC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively[5]. |
| IC50& Target[1][2] | PKC 8.5 μM (IC50) | Topoisomerase II |
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体外研究
(In Vitro) | Mitoxantrone dihydrochloride inhibits PKC in a competitive manner with respect to histone H1, and its Kivalue is 6.3 μM and in a non-competitive manner with respect to phosphatidylserine and ATP[1].
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[2].
Mitoxantrone dihydrochloride shows cytotoxicity to human breast carcinoma cell lines MDA-MB-231 and MCF-7 with IC50values of 18 and 196 nM, respectively[3].
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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[4].
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[4].
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 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) |
| 溶解性数据 | In Vitro: H2O : 100 mg/mL(193.27 mM;Need ultrasonic) DMSO : ≥ 43 mg/mL(83.11 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 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 |
*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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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. 请依序添加每种溶剂： 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。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： PBS Solubility: 2 mg/mL (3.87 mM); Clear solution; Need ultrasonic and warming and heat to 60℃ *以上所有助溶剂都可在本网站选购。
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