Size | Price | Stock | Qty |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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Purity: ≥98%
Mitoxantrone HCl (formerly NSC-301739; NSC301739; DHAQ; CL-232325; Mitroxone; Neotalem; Onkotrone; Pralifan; Novantrone), the hydrochloride salt of Mitoxantrone which is an anthracenedione anticancer agent, is a potent type II topoisomerase inhibitor with potential antitumor activity. It has an IC50 of 2.0 μM in HepG2 and 0.42 mM in MCF-7/wt cells for TOPO II inhibition. It is a confirmed treatment for multiple sclerosis and an anti-neoplastic for leukemia and other cancers. By preventing DNA synthesis and the division of cells, mitoxantrone suppressed leukemia. It impacted several immune cells, including macrophages, T cells, and B cells, among others. Numerous DSBs (DNA strand breaks), chromatin structure alterations, and other events were caused by its interference with TOPO-II-mediated DNA cleavage.
Targets |
PKC ( IC50 = 8.5 μM ); Topoisomerase II
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
Mitoxantrone inhibits PKC in a non-competitive manner with respect to phosphatidylserine and ATP, but in a competitive manner with respect to histone H1, where its Ki value is 6.3 μM. Cell viability is reduced when B-CLL cells are treated with mitoxantrone (0.5 μg/mL) for 48 hours. Poly(ADP-ribose) polymerase (PARP) is subjected to proteolytic cleavage and DNA fragmentation upon induction by mitoxantrone, indicating that the cytotoxic effect of the drug is a result of apoptosis induction. Human breast carcinoma cell lines MDA-MB-231 and MCF-7 exhibit cytotoxicity to mitoxantrone, with IC50 values of 18 and 196 nM, respectively.
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Cell Assay |
In standard 96-well plates, the human breast carcinoma cell lines MDA-MB-231 and MCF-7 are seeded. The culture medium is swapped out for one containing varying concentrations of mitoxantrone (10-5 to 5 μM) with or without DHA (30 μM) for a period of seven days following seeding. The tetrazolium salt assay is used to determine the overall viability of cells.
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Animal Protocol |
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References | |||
Additional Infomation |
Mitoxantrone, a synthetic anthracenedione, was developed in the 1980s as a doxorubicin analogue in a program to find a cytotoxic agent with decreased cardiotoxicity compared with doxorubicin. It was approved by the FDA in 1987 for the treatment of adult acute myeloid leukemia and in 1996 for symptomatic hormone-refractory prostate cancer. In 2000, mitoxantrone was approved by the FDA for the treatment of worsening relapsing-remitting multiple sclerosis (MS), secondary progressive MS, and progressive-relapsing MS. Mitoxantrone is taken up rapidly by tissues, from which it is released slowly, and the terminal half-life ranges from 8.9 hours to 9 days. The highest concentrations of the drug are typically found in the thyroid, liver, and heart, and the drug persists in the body for as long as 272 days. Mitoxantrone is effective in reducing disease progression through a variety of different mechanisms of action. For example, it suppresses the proliferation of T cells, B cells, and macrophages. It impairs antigen presentation and decreases the secretion of proinflammatory cytokines. Mitoxantrone enhances T-cell suppressor function and inhibits B-cell function and antibody production. Finally, it inhibits macrophage-mediated myelin degradation. Compared with interferon betas, mitoxantrone has a broad range of actions and has effects on many different types of immune cells.[2]
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Molecular Formula |
C22H29CLN4O6.HCL
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Molecular Weight |
517.4
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Exact Mass |
516.15
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Elemental Analysis |
C, 51.07; H, 5.84; Cl, 13.70; N, 10.83; O, 18.55
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CAS # |
70476-82-3
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Related CAS # |
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PubChem CID |
51082
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Appearance |
Black solid powder
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Boiling Point |
805.7ºC at 760 mmHg
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Melting Point |
203-205ºC
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Flash Point |
441.1ºC
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LogP |
2.4
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tPSA |
163.18
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SMILES |
C1=CC(=C2C(=C1NCCNCCO)C(=O)C3=C(C=CC(=C3C2=O)O)O)NCCNCCO.Cl.Cl
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InChi Key |
ZAHQPTJLOCWVPG-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C22H28N4O6.2ClH/c27-11-9-23-5-7-25-13-1-2-14(26-8-6-24-10-12-28)18-17(13)21(31)19-15(29)3-4-16(30)20(19)22(18)32;;/h1-4,23-30H,5-12H2;2*1H
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Chemical Name |
1,4-dihydroxy-5,8-bis[2-(2-hydroxyethylamino)ethylamino]anthracene-9,10-dione;dihydrochloride
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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
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.83 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.83 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: Saline: 30 mg/mL Solubility in Formulation 4: 2 mg/mL (3.87 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9327 mL | 9.6637 mL | 19.3274 mL | |
5 mM | 0.3865 mL | 1.9327 mL | 3.8655 mL | |
10 mM | 0.1933 mL | 0.9664 mL | 1.9327 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT04330820 | Active Recruiting |
Drug: Venetoclax Oral Tablet | Relapsed Adult AML Refractory AML |
Technische Universität Dresden | April 6, 2020 | Phase 1 Phase 2 |
NCT02553460 | Active Recruiting |
Drug: Mitoxantrone Drug: ITMHA |
Acute Lymphoblastic Leukemia | St. Jude Children's Research Hospital |
January 29, 2016 | Phase 1 Phase 2 |
NCT03026842 | Active Recruiting |
Drug: Mitoxantrone, Cytarabine Drug: Decitabine |
Acute Myeloid Leukemia | The First Hospital of Jilin University |
January 2017 | Phase 4 |
NCT03441048 | Active Recruiting |
Drug: Mitoxantrone Drug: G-CSF |
Acute Myeloid Leukemia | Medical College of Wisconsin | May 22, 2018 | Phase 1 |
NCT04719065 | Recruiting | Drug: Mitoxantrone Hydrochloride Liposome, intravenous injection (IV) |
Advanced Solid Tumor | CSPC ZhongQi Pharmaceutical Technology Co., Ltd. |
January 13, 2021 | Phase 1 |