Mitoxantrone 是一种有效的拓扑异构酶II (topoisomerase II) 抑制剂。Mitoxantrone 也可抑制蛋白激酶 C (PKC),其IC50值为 8.5 μM。Mitoxantrone 诱导 B- 慢性淋巴细胞白血病 (B-CLL) 细胞凋亡 (apoptosis)。Mitoxantrone 具有抗肿瘤活性。Mitoxantrone 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 is a potenttopoisomeraseIIinhibitor. Mitoxantrone also inhibits protein kinase C (PKC) activity with anIC50of 8.5 μM. Mitoxantrone inducesapoptosisof B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone shows antitumor activity[1][2][3][4]. Mitoxantrone 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 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 (0.5 μg/mL, 48 h) induces a decrease in B-CLL cells. Mitoxantrone induces DNA fragmentation and the proteolytic cleavage of poly(ADP-ribose) polymerase (PARP), demonstrating that the cytotoxic effect of Mitoxantrone is due to induction of apoptosis[2]. Mitoxantrone 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 (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 (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 | -20°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
溶解性数据 | In Vitro: DMSO : 62.5 mg/mL(140.61 mM;Need ultrasonic) 配制储备液 1 mM | 2.2498 mL | 11.2491 mL | 22.4982 mL | 5 mM | 0.4500 mL | 2.2498 mL | 4.4996 mL | 10 mM | 0.2250 mL | 1.1249 mL | 2.2498 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 (protect from 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: ≥ 2.08 mg/mL (4.68 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.68 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 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: ≥ 2.08 mg/mL (4.68 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.68 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 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。 *以上所有助溶剂都可在本网站选购。
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