| Field | Specification |
|---|---|
| Target | |
| Alternative names | Mitozantrone; NSC 301739 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C22H28N4O6 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Mitoxantrone, also known as Mitozantrone or NSC 301739, is a potent topoisomerase II inhibitor that also inhibits protein kinase C (PKC) activity, with an IC50 of 8.5 μM. It induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells and shows antitumor activity[1][2][3][4]. It also has anti-orthopoxvirus activity, with EC50s of 0.25 μM and 0.8 μM for cowpox and monkeypox, respectively[5]. It is supplied as a dark blue to black solid (C22H28N4O6, MW 444.48) at 99.58% purity.
Physical & Chemical Properties
| CAS Number | 65271-80-9 |
|---|---|
| Molecular Formula | C22H28N4O6 |
| Molecular Weight | 444.48 g/mol |
| Purity | 99.58% |
| Appearance | Solid |
| Color | Dark blue to black |
| SMILES | O=C1C2=C(C(NCCNCCO)=CC=C2NCCNCCO)C(C3=C(O)C=CC(O)=C13)=O |
| Target | PKC, Topoisomerase II |
| Signaling Pathway | Cell Cycle/DNA Damage; TGF-beta/Smad; Epigenetics; Anti-infection; Apoptosis |
| Solubility | In Vitro: DMSO: 35 mg/mL (78.74 mM; Requires sonication and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | -20°C, protect from light. In solvent: -80°C, 6 months; -20°C, 1 month (protect from light). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
[1][2]
|
PKC 8.5 μM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 35 mg/mL (78.74 mM) | requires sonication and warming and heat to 60°C; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); protect from light; avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.08 mg/mL (4.68 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.08 mg/mL (4.68 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Data provided by the manufacturer.
In Vitro
Mitoxantrone inhibits PKC competitively with respect to histone H1, with a Ki of 6.3 μM, and noncompetitively with respect to phosphatidylserine and ATP[1]. Mitoxantrone (0.5 μg/mL, 48 h) reduces B-CLL cells. Mitoxantrone induces DNA fragmentation and proteolytic cleavage of poly(ADP-ribose) polymerase (PARP), which shows that Mitoxantrone cytotoxicity results from apoptosis induction[2]. Mitoxantrone shows cytotoxicity toward MDA-MB-231 and MCF-7 human breast carcinoma cells, with IC50 values of 18 and 196 nM, respectively[3].
In Vivo
In mice with IP implanted L1210 leukemia, Mitoxantrone (IP, 0-3.2 mg/kg/day) yields a statistically significant number of 60-day survivors at 1.6 mg/kg[4]. In SC implanted Lewis lung carcinoma, Mitoxantrone (IV, 0-3.2 mg/kg/day) displays effective antitumor activity and gives a 60% ILS (increase in lifespan) at 3.2 mg/kg[4].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Cell Assay[3]
Seed MDA-MB-231 and MCF-7 human breast carcinoma cells in standard 96-well plates. One day after seeding, replace the culture medium with medium containing different concentrations of Mitoxantrone (10-5 to 5 μM), with or without DHA (30 μM), for 7 days. Measure cell viability overall by tetrazolium salt assay[3].
Animal Administration[4]
Mice: Test Mitoxantrone for antitumor activity against experimental tumors in mice and compare the results with those of seven antitumor antibiotics. Give the drugs IP or IV, generally on days 1, 5, and 9 following tumor inoculation. Give Mitoxantrone IP at the optimal dose (1.6 mg/kg/day; as a free base)[4].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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