您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > Mitoxantrone HCl(mitozantrone)
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Mitoxantrone HCl(mitozantrone)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Mitoxantrone HCl(mitozantrone)图片
CAS NO:70476-82-3
规格:≥98%
包装与价格:
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
5g电议
10g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)517.4
FormulaC22H29ClN4O6.HCl
CAS No.70476-82-3 (HCl salt);
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; CL-232325; NSC301739; CL 232325; NSC 301739; DHAQ; CL232325; Mitozantrone; Mitoxantrone HCl; Mitoxantrone dihydrchloride; US brand name: Novantrone. NSC 301739; DHAQ; CL232325; Foreign brand names: Mitroxone; Neotalem; Onkotrone; Pralifan;

Chemical Name: 1,4-dihydroxy-5,8-bis((2-((2-hydroxyethyl)amino)ethyl)amino)anthracene-9,10-dione dihydrochloride

SMILES Code: O=C1C2=C(C(NCCNCCO)=CC=C2NCCNCCO)C(C3=C(O)C=CC(O)=C13)=O.[H]Cl.[H]Cl

实验参考方法
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: Mitoxantrone inhibits PKC in a competitive manner with respect to histone H1, and its Ki value is 6.3 μM and in a non-competitive manner with respect to phosphatidylserine and ATP. Treatment of B-CLL cells for 48 h with mitoxantrone (0.5 μg/mL) induces a decrease in cell viability. Mitoxantrone induces DNA fragmentation and the proteolytic cleavage of poly(ADP-ribose) polymerase (PARP), demonstrating that the cytotoxic effect of mitoxantrone is due to induction of apoptosis. Mitoxantrone shows cytotoxicity to human breast carcinoma cell lines MDA-MB-231 and MCF-7 with IC50 values of 18 and 196 nM, respectively.


Cell Assay: 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.

In Vivo Mitoxantrone given IP at the optimal dose (1.6 mg/kg/day; as a free base) produces a statistically significant number of 60-day survivors (curative effect) in mice with IP implanted L1210 leukemia. In SC implanted Lewis lung carcinoma, mitoxantrone and ADM administered IV also shows effective antitumor activities and produces a 60% and a 45% ILS, respectively.
Animal model Mice
Formulation & Dosage 1.6 mg/kg/day; i.p. or i.v.
ReferencesCurr Opin Rheumatol. 1999 May;11(3):226-32; Arthritis Rheum. 1989 Sep;32(9):1065-73; Cancer Chemother Pharmacol. 1982;8(2):157-62.