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Mitoxantrone dihydrochloride

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Chemical Structure| 70476-82-3 同义名 : 米托蒽醌二盐酸盐 ;Mitozantrone dihydrochloride;NSC 301739 dihydrochloride;NSC 301739;NCI 301739;Mitoxantrone (hydrochloride);Mitozantrone 2HCl;NSC-301739 2HCl;Mitoxantrone 2HCl
CAS号 : 70476-82-3
货号 : A166750
分子式 : C22H30Cl2N4O6
纯度 : 98%
分子量 : 517.4
MDL号 : MFCD00242943
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(57.98 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

H2O: 100 mg/mL(193.27 mM)，配合低频超声助溶
动物实验配方：

PO 0.5% CMC-Na 30 mg/mL suspension

生物活性
靶点

  • Topo II
描述 Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. It is also showed inhibitory effect on protein kinase C (PKC) activity with IC50=8.5μM. Mitoxantrone inhibited PKC in a competitive manner with respect to histone H1 (Ki=6.3μM) and in a non-competitive manner with respect to phophatidylserine and ATP[3]. 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[4]. 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[5].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
A2780-cell Growth inhibition assay Concentration required to inhibit A2780-cell growth by 50%, IC50=0.55 nM 9703471
A549 cells Function assay Activity against A549 cancer cell line, IC50=3.1 nM 8960558
CCRF-CEM cells Cytotoxicity assay 48 h Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay, IC50=0.036 μM 22582991
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
NCT00004001 Prostate Cancer Phase 3 Completed - United States, Arizona ... 展开 >> CCOP - Scottsdale Oncology Program Scottsdale, Arizona, United States, 85259-5404 United States, Florida Mayo Clinic Jacksonville, Florida, United States, 32224 United States, Illinois CCOP - Illinois Oncology Research Association Peoria, Illinois, United States, 61602 CCOP - Carle Cancer Center Urbana, Illinois, United States, 61801 United States, Iowa CCOP - Cedar Rapids Oncology Project Cedar Rapids, Iowa, United States, 52403-1206 CCOP - Iowa Oncology Research Association Des Moines, Iowa, United States, 50309-1016 Siouxland Hematology-Oncology Sioux City, Iowa, United States, 51101-1733 United States, Minnesota Mayo Clinic Cancer Center Rochester, Minnesota, United States, 55905 CentraCare Health Plaza Saint Cloud, Minnesota, United States, 56303 United States, Nebraska CCOP - Missouri Valley Cancer Consortium Omaha, Nebraska, United States, 68106 United States, North Dakota Medcenter One Health System Bismarck, North Dakota, United States, 58501 CCOP - Merit Care Hospital Fargo, North Dakota, United States, 58122 Altru Health System Grand Forks, North Dakota, United States, 58201 United States, Pennsylvania CCOP - Geisinger Clinic and Medical Center Danville, Pennsylvania, United States, 17822-2001 United States, South Dakota Rapid City Regional Hospital Rapid City, South Dakota, United States, 57709 CCOP - Sioux Community Cancer Consortium Sioux Falls, South Dakota, United States, 57104 收起 <<
NCT00002498 Breast Cancer Phase 2 Unknown - Netherlands ... 展开 >> Leiden University Medical Center Leiden, Netherlands, 2300 ZA St. Radboud University Hospital Nijmegen, Netherlands, 6500 HB 收起 <<
NCT00219908 Relapsing-Remitting Multiple S... 展开 >>clerosis 收起 << Phase 2 Terminated - France ... 展开 >> Hôpital Cote de Nacre Caen, France, 14033 Hôpital Gabriel Montpied Clermont-Ferrand, France, 63003 CHU Henri Mondor Creteil, France, 94000 Hôpital Général Dijon, France, 21033 CHU Limoges Limoges, France, 87042 Institut Catholique de Lille Lomme, France, 59462 Pierre Weitheimer Hospital Lyon, France, 69394 Chu Timone Marseille, France, 13385 Centre Guy de Chauliac Montpellier, France, 34295 CHU Hôpital Central Nancy, France, 54035 CHU Nice, France, 06000 CHU Pitié-Salpétrière Paris, France, 75013 Hôpital Saint-Anne Paris, France, 75014 Centre Fondation Rotschild Paris, France, 75019 Tenon Hospital Paris, France, 759170 CHU Strasbourg Strasbourg, France, 67000 CHU Purpan Toulouse, France, 31059 Italy Psichiatriche dell'Università di Bari, Policlinico Bari, Italy, 70122 Dipartimento di Scienze Neurologiche e Psichiatriche Firenze, Italy, 50134 Hospedal Civile Gallarate, Italy, 21013 Neuroriabilitazione dell'Università Genova, Italy, 16132 Fondazionz SAN Raffaele del monte tabor Milano, Italy, 20132 Clinica Neurologica Università di Torino Torino, Italy, 10126 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.93mL

0.39mL

0.19mL

9.66mL

1.93mL

0.97mL

19.33mL

3.87mL

1.93mL
参考文献

[1]Seitz M. Molecular and cellular effects of methotrexate. Curr Opin Rheumatol. 1999 May;11(3):226-32.

[2]Hirata S, Matsubara T, et al. Inhibition of in vitro vascular endothelial cell proliferation and in vivo neovascularization by low-dose methotrexate. Arthritis Rheum. 1989 Sep;32(9):1065-73.

[3]Takeuchi N, Nakamura T, Takeuchi F, Hashimoto E, Yamamura H. Inhibitory effect of mitoxantrone on activity of protein kinase C and growth of HL60 cells. J Biochem. 1992;112(6):762-767.

[4]Bellosillo B, Colomer D, Pons G, Gil J. Mitoxantrone, a topoisomerase II inhibitor, induces apoptosis of B-chronic lymphocytic leukaemia cells. Br J Haematol. 1998;100(1):142-146. 

[5]Fujimoto S, Ogawa M. Antitumor activity of mitoxantrone against murine experimental tumors: comparative analysis against various antitumor antibiotics. Cancer Chemother Pharmacol. 1982;8(2):157-162.