| CAS |
70476-82-3 |
| Chinese Name |
米托蒽醌二盐酸盐 |
| English Name |
Mitoxantrone HCl |
| Synonyms |
盐酸米托蒽醌;mitozantrone dihydrochloride;NSC-301739 |
| Molecular Formula |
C22H28N4O6·2HCl |
| Molecular Weight |
517.4 |
| Solubility |
Soluble in Water/DMSO ≥5mg/mL |
| Purity |
HPLC≥98% |
| Appearance |
Blue-black Solid |
| Storage |
Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 274-619-1 |
| MDL |
MFCD00242943 |
| SMILES |
O=C1C2=C(C(NCCNCCO)=CC=C2NCCNCCO)C(C3=C(O)C=CC(O)=C13)=O.[H]Cl.[H]Cl |
| InChIKey |
ZAHQPTJLOCWVPG-UHFFFAOYSA-N |
| InChI |
InChI=1S/C22H28N4O6.2ClH/c27-11-9-23-5-7-25-13-1-2-14(26-8-6-24-10-12-28)18-17(13)21(31)19-15(29)3-4-16(30)20(19)22(18)32;;/h1-4,23-30H,5-12H2;2*1H |
| PubChem CID |
51082 |
| Target Point |
Topoisomerase;PKC |
| Passage |
DNA Damage/DNA Repair;TGF-beta/Smad;Epigenetics |
| Background |
Mitoxantrone HCl is an inhibitor of topoisomerase II; also inhibits protein kinase C (PKC). |
| Biological Activity |
Mitoxantrone dihydrochloride是拓扑异构酶II (topoisomerase II)的抑制剂；也可抑制蛋白激酶C (PKC)， IC50值为8.5 μM。[1-4] |
| In Vitro |
米托蒽醌以相对于组蛋白H1的竞争性方式抑制PKC，并且其Ki值为6.3μM并且以非竞争性方式相对于磷脂酰丝氨酸和ATP [1]。用米托蒽醌(0.5μg/ mL)处理B-CLL细胞48小时诱导细胞活力降低。米托蒽醌诱导DNA片段化和聚(ADP-核糖)聚合酶(PARP)的蛋白水解切割，证明米托蒽醌的细胞毒性作用是由于诱导细胞凋亡[2]。米托蒽醌显示对人乳腺癌细胞系MDA-MB-231和MCF-7的细胞毒性，IC50值分别为18和196 nM [3]。 |
| In Vivo |
米托蒽醌以最佳剂量(1.6mg/kg /天;作为游离碱)给予IP，在IP植入L1210白血病的小鼠中产生统计学上显著数量的60天存活者(疗效)。在SC植入Lewis肺癌中，米托蒽醌和静脉注射ADM也显示出有效的抗肿瘤活性，分别产生60％和45％的ILS [4]。 |
| Cell Experiment |
将人乳腺癌细胞系MDA-MB-231和MCF-7接种在标准96孔板中。接种后一天，更换培养基，并在7天内用含有或不含DHA(30μM)的不同浓度的米托蒽醌(10-5至5μM)的培养基替换。通过四唑盐测定[3]整体测量细胞活力。 |
| Animal Experiment |
小鼠：测试米托蒽醌对小鼠中实验性肿瘤的抗肿瘤活性，并将结果与七种抗肿瘤抗生素的结果进行比较。通常在肿瘤接种后第1，5和9天给予IP或IV的药物。米托蒽醌以最佳剂量(1.6mg/kg /天;作为游离碱)给予IP [4]。 |
| Data Literature Source |
[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]. 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.
[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 |
| Unit |
Bottle |
| Specification |
50mg 10mM*1mL in DMSO 100mg |
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