| Description | Mitoxantrone dihydrochloride (NSC-301739) is the hydrochloride salt of an anthracenedione antibiotic with antineoplastic activity. It is a type II topoisomerase inhibitor. |
| In vitro | Methotrexate在小鼠气囊炎模型中,Methotrexate的IC50 为每周0.08 mg/kg. |
| In vivo | 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。 |
| Cell experiments | 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]. |
| Target activity | PKC:8.5 μM |
| Synonyms | 米托蒽醌二盐酸盐, 盐酸米托蒽醌, Mitoxantrone 2HCl, Mitoxantrone hydrochloride, NSC-301739, mitozantrone dihydrochloride |
| molecular weight | 517.4 |
| Molecular formula | C22H30Cl2N4O6 |
| CAS | 70476-82-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 38.8 mg/mL (75 mM) H2O: 2.6 mg/mL (5 mM) |
| References | 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. |