Mitoxantrone dihydrochloride

Mitoxantrone dihydrochloride (NSC-301739) 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。

CAS号

70476-82-3

分子式

C22H30Cl2N4O6

主要靶点

Topoisomerase|PKC

仅限科研使用

Cat No : CM06710

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Synonyms

米托蒽醌二盐酸盐|盐酸米托蒽醌|Mitoxantrone 2HCl|mitozantrone dihydrochloride|Mitoxantrone hydrochloride|NSC-301739



产品信息

Mitoxantrone dihydrochloride (NSC-301739) is the hydrochloride salt of an anthracenedione antibiotic with antineoplastic activity. It is a type II topoisomerase inhibitor.

CAS号 70476-82-3
分子式 C22H30Cl2N4O6
主要靶点 Topoisomerase|PKC
主要通路 DNA损伤和修复|表观遗传|细胞骨架
分子量 517.4
纯度 97.81%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 米托蒽醌二盐酸盐|盐酸米托蒽醌|Mitoxantrone 2HCl|mitozantrone dihydrochloride|Mitoxantrone hydrochloride|NSC-301739

靶点活性

kinase C (PKC):8.5 μM

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。

体外活性

Methotrexate在小鼠气囊炎模型中,Methotrexate的IC50 为每周0.08 mg/kg.

溶解度

H2O:2.6 mg/mL (5 mM),DMSO:38.8 mg/mL (75 mM)

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].

参考文献

1.Seitz M. Curr Opin Rheumatol, 1999, 11(3), 226-232.
2.Hirata S, et al. Arthritis Rheum, 1989, 32(9), 1065-1073.
3.Segal R, et al. Semin Arthritis Rheum, 1990, 20(3), 190-200.
4.Genestier L, et al. J Clin Invest, 1998, 102(2), 322-328.
5.Cronstein BN, et al. J Clin Invest, 1993, 92(6):2675-2682.

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