product name Mitoxantrone HCl
Description: Mitoxantrone (also known as NSC-301739) is a type II topoisomerase inhibitor with IC50 of 2.0 μM, 0.42 mM for HepG2 and MCF-7/wt cells, respectively. It is used as an anti-neoplastic drug for leukemia and other types of cancer, and a proven drug for multiple sclerosis. Mitoxantrone suppressed the leukemia via inhibiting DNA synthesis and cell cycle progression. It had effect on different immune cells (e.g. T cell, B cell and macrophage etc.). It interfered with TOPO-II-mediated DNA cleavage and led to multiple DSB (DNA strand breaks), chromatin structure changes etc.
References: Curr Opin Rheumatol. 1999 May;11(3):226-32; Neurology. 2004 Dec 28;63(12 Suppl 6):S15-8.
517.4
Formula
C22H29ClN4O6.HCl
CAS No.
70476-82-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 89 mg/mL (172.0 mM)
Water: 89 mg/mL (172.0 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
Saline: 30 mg/mL
Synonyms
NSC-301739
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Curr Opin Rheumatol. 1999 May;11(3):226-32; Arthritis Rheum. 1989 Sep;32(9):1065-73. |
