Mitoxantrone hydrochloride 是一种拓扑异构酶 II 的抑制剂;也可抑制蛋白激酶C (PKC),IC50值为8.5 μM。
产品描述
Mitoxantrone Hydrochloride is the hydrochloride salt of an anthracenedione antibiotic with antineoplastic activity. It is a type II topoisomerase inhibitor.
体外活性
Methotrexate在小鼠气囊炎模型中,Methotrexate的IC50 为每周0.08 mg/kg.
体内活性
Methotrexate能够抑制嘌呤和嘧啶的从头合成,多胺的形成以及DNA、RNA、磷脂和蛋白质的转甲基作用。Methotrexate抑制胸苷酸合成酶,使细胞内胸苷酸不足,最终导致抗增殖的细胞毒性作用。Methotrexate通过主动转运或易化扩散进入细胞,在细胞内经过多聚谷氨酸化后,会抑制二氢叶酸还原酶和二氢叶酸转化为四氢叶酸。
细胞实验
The human breast carcinoma cell lines MDA-MB-231 and MCF-7 are seeded in standard 96-well plates. One day after seeding, the culture medium is changed and replaced by medium containing different concentration of Mitoxantrone (10-5 to 5 μM) with or without DHA (30 μM) during 7 days. Viability of cells are measured as a whole by the tetrazolium salt assay[3].
Cas No.
70476-82-3
分子式
C22H30Cl2N4O6
分子量
517.4
别名
盐酸米托蒽醌;NSC-301739;Mitoxantrone 2HCl;mitozantrone dihydrochloride;Mitoxantrone hydrochloride;米托蒽醌二盐酸盐
储存和溶解度
DMSO:38.8 mg/mL (75 mM)
H2O:2.6 mg/mL (5 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years