米托蒽醌二盐酸盐, DNA 拓扑异构酶 II alpha 抑制剂

1,4-dihydroxy-5,8-bis(2-(2-hydroxyethylamino)ethylamino)anthracene-9,10-dione dihydrochloride

Mitoxantrone (NSC-301739) 2HCl

M408662-1ml

1ml

10mM in DMSO

-80℃储存

超低温冰袋运输

Information Mitoxantrone 2HCl (NSC-301739) is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor oftype II topoisomeraseandprotein kinase C (PKC)with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 In vitro Mitoxantrone induces DNA fragmentation and the proteolytic cleavage of poly(ADP-ribose) polymerase (PARP), a marker of the activation of caspases, in all the patients studied, demonstrating that the cytotoxic effect of mitoxantrone is due to induction of apoptosis. Mitoxantrone activates NFkappaB and stimulates IkappaBalpha degradation in the promyelocytic leukemia cell line HL60 but not in the variant cells, HL60/MX2 cells, which lack the beta isoform of topoisomerase II and express a truncated alpha isoform that results in an altered subcellular distribution. Mitoxantrone inhibits proliferation of activated PBMCs, B lymphocytes, or antigen-specific T-cell lines (TCLs) stimulated on antigen-presenting cells (APCs) in a dose-dependent manner. Mitoxantrone induces apoptosis of PBMCs, monocytes and DCs at low concentrations, whereas higher doses causes cell lysis. In vivo Mitoxantrone transiently decreases the growth rate of HID xenografts in mice but does not affect that of PAC120 xenografts. Mitoxantrone results in the severity of the cardiac lesions and the nephropathy and the intestinal toxicity in spontaneously hypertensive rats. Mitoxantrone and iron(III) form a strong 2:1 complex, in which mitoxantrone may be acting as a tridentate ligand. Cell Data cell lines： Concentrations： Incubation Time： Powder Purity:≥95%

Mitoxantrone 2HCl (NSC-301739) 是 Mitoxantrone 的二盐酸盐。米托蒽醌是 II 型拓扑异构酶和蛋白激酶 C (PKC) 的抑制剂，对 PKC 的 IC50 值为 8.5 μM。米托蒽醌可抑制 MCF-7/wt 细胞的增殖生长，IC50 为 0.42 μM。米托蒽醌还能诱导细胞凋亡。

70476-82-3(DMSO)

C22H29ClN4O6·2HCl

517.4 g/mol

Cl.Cl.OCCNCCNC1=CC=C(NCCNCCO)C2=C1C(=O)C3=C(O)C=CC(=C3C2=O)O

Solubility (25°C) In vitro DMSO: 4.89 mg/mL (37.85 mM);

抑制剂

DNA 拓扑异构酶 II alpha 抑制剂