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Mitoxantrone Topoisomerase inhibitor

Name: Mitoxantrone
Brand: Selleck Chemicals
SKU: S1889
Availability: InStock
Rating: 5 (8 reviews)

Cat.No.S1889

Mitoxantrone is a type II topoisomerase inhibitor with IC50 of 2.0 μM, 0.42 mM for HepG2 and MCF-7/wt cells, respectively.

Chemical Structure

Molecular Weight: 444.48

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Quality Control

Batch: Purity: 99.27%

99.27

Related Targets	CDK HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Aurora Kinase
Other Topoisomerase Inhibitors	Camptothecin (CPT) Betulinic acid Beta-Lapachone (S)-10-Hydroxycamptothecin Amonafide Ellagic acid Voreloxin (SNS-595) hydrochloride Cu(II)-Elesclomol Hydroxy Camptothecine Rubitecan

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description
L1210 cell	Cytotoxic assay	48 h	Cytotoxic potency required to inhibit L1210 cell growth by 50% after cell drug contact for 48 hrs, IC50=4e-05 μM
human HL60 cells	Cytotoxic assay	48 h	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay, GI50=0.33 nM
MDA435/LCC6 cells	Proliferation assay		Antiproliferative activity against MDA435/LCC6 cells by ELISA, IC50=0.35 nM
A2780-cell	Growth inhibition assay		Concentration required to inhibit A2780-cell growth by 50%, IC50=0.55 μM
A2780 cell	Cytotoxic assay	96 h	Cytotoxic potency required to inhibit A2780 cell growth by 50% after cell drug contact for 96 hrs, IC50=0.55 nM
G-361 cell	Cytotoxic assay		Cytotoxic potency required to inhibit G-361 cell growth by 50%, IC50=0.65 nM
HL60 human leukemia cell	Cytotoxic assay	72 h	Compound was tested in vitro for cytotoxicity against HL60 human leukemia cell line (72 hr exposure to compound), IC50=0.81 nM
human HL60 cells	Proliferation assay	72 h	Antiproliferative activity against human HL60 cells after 72 hrs by SRB assay, IC50=2.5 nM
human K562 cells	Cytotoxic assay	5 days	Cytotoxicity against human K562 cells after 5 days by XTT assay, IC50=2.6 nM
CH1-cell	Growth inhibition assay		Concentration required to inhibit CH1-cell growth by 50%, IC50=2.65 nM
uterine sarcoma MES-SA cells	Cytotoxic assay		In vitro cytotoxicity against uterine sarcoma MES-SA cells, IC5=3 nM
MES-SA cells	Proliferation assay	72 h	Antiproliferative activity against MES-SA cells by MTT assay after 72 hrs, IC50=3 nM
A549 cells	Function assay		Tested for inhibitory activity against human tumor cell line A549 (a non small, drug resistant cell line that does not produce P-glycoprotein) of lung carcinoma using sulforhodamine B assay, IC50=3 nM
human LoVo cancer cell	Cytotoxic assay	144 h	Cytotoxicity against human LoVo cancer cell line was determined after 144 hr, IC50=3.3 nM
P388 cells	Proliferation assay		Antiproliferative activity against P388 cells by ELISA, IC50=4.3 nM
MCF-7	Growth inhibition assay		In vitro inhibition of tumor cell growth in the human mammary tumor MCF-7 system, IC50=5 nM
murine L1210 sensitive cell line	Function assay		Anti-tumor activity against murine L1210 sensitive cell line by using MTT assay, IC50=5 nM
human Daudi cells	Proliferation assay	72 h	Antiproliferative activity against human Daudi cells after 72 hrs by MTT assay, IC50=5 nM
SKOV-3-cell	Growth inhibition assay		Concentration required to inhibit SKOV-3-cell growth by 50%, IC50=5.3 nM
human cell line DU145	Cytotoxic assay		In vitro Cytotoxic activity of compound in comparison with reference compounds in human cell line DU145, IC50=5.6 nM
human HCT116 cancer cell line	Cytotoxic assay	144 h	Cytotoxicity against human HCT116 cancer cell line was determined after 144 hr, IC50=5.8 nM
OVCAR-3 cell	Function assay		Inhibitory activity against OVCAR-3 cell line, IC50=5.8 nM
human MES-SA cells	Proliferation assay	72 h	Antiproliferative activity against human MES-SA cells after 72 hrs by MTT assay, IC50=6 nM
human PC3 cancer cell	Cytotoxic assay	144 h	Cytotoxicity against human PC3 cancer cell line was determined after 144 hr, IC50=7 nM
MDR cell line K562R	Cytotoxic assay	72 h	Compound was tested in vitro for cytotoxicity against MDR cell line K562R (72 hr exposure to compound), IC50=7.06 nM
WiDr cell	Function assay		Activity against human colon carcinoma sensitive WiDr cell line, IC50=8.1 nM
MXF7 breast cell line	Function assay		Antitumor activity against human mammary carcinoma sensitive MXF7 breast cell line, IC50=8.7 nM
HT-29 cell	Cytotoxic assay		In vitro cytotoxicity was tested against human colon adenocarcinoma HT-29 cell line, IC50=0.01 μM
CHO cell line xrs6	Cytotoxic assay		Cytotoxicity against CHO cell line xrs6, IC50=0.01 μM
human HL60 cells	Growth inhibition assay		Growth inhibition of human HL60 cells by Almar blue assay, GI50=0.01 μM
HT-29 cells	Cytotoxic assay		Cytotoxicity is determined as the concentration required to inhibit the growth of human colon adenocarcinoma (HT-29) cell line, IC50=0.01 μM
human Ishikawa cells	Proliferation assay	72 h	Antiproliferative activity against human Ishikawa cells after 72 hrs by MTT assay, IC50=0.01 μM
HEK293 cells	Cytotoxic assay	72 h	Cytotoxicity against HEK293 cells after 72 hrs by MTT assay, IC50=0.01 μM
human MKN45 cancer cell	Cytotoxic assay	144 h	Cytotoxicity against human MKN45 cancer cell line was determined after 144 hr, IC50=0.012 μM
human LoVo cancer cell	Cytotoxic assay	1 h	Cytotoxicity against human LoVo cancer cell line was determined after 1 hr, IC50=0.012 μM
human FM3 cells	Proliferation assay	72 h	Antiproliferative activity against human FM3 cells after 72 hrs by MTT assay, IC50=0.013 μM
human HL60 cells	Cytotoxic assay	48 h	Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by celltiter-blue assay, IC50=0.016 μM
SK-BR-3 cells	Function assay		The IC50 value was measured on human breast cancer cell line SK-BR-3, IC50=0.016 μM
human small-cell lung cancer (SCLC)	Cytotoxic assay		Cytotoxicity against human small-cell lung cancer (SCLC), IC50=0.02 μM
human HCT116 cells	Cytotoxic assay	72 h	Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50=0.022 μM
human HCT116 cells	Proliferation assay	72 h	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50=0.025 μM
A0375 cells	Function assay		Inhibitory activity against human tumor cell line A0375 melanoma, IC50=0.026 μM
NCI-H460 cells	Cytotoxic assay	48 h	Cytotoxicity against human NCI-H460 cells after 48 hrs by resazurin dye assay, EC50=0.03 μM
CCRF-CEM cells	Cytotoxic assay	48 h	Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay, IC50=0.036 μM
human HeLa cells	Proliferation assay	72 h	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay, IC50=0.044 μM
human NCI60 cells	Function assay	48 h	Antitumor activity against human NCI60 cells after 48 hrs by SRB assay, GI50=0.04786 μM
UA375 cells	Function assay		Tested for inhibitory activity against human tumor cell line UA375 of melanoma using sulforhodamine B assay, IC50=0.048 μM
HT1080 cells	Function assay		Inhibitory activity against human tumor cell line HT1080, IC50=0.066 μM
human MES-SA/Dx5 cells	Proliferation assay	72 h	Antiproliferative activity against human MES-SA/Dx5 cells after 72 hrs by MTT assay, IC50=0.073 μM
human RKOp27 cells	Proliferation assay	48 h	Antiproliferative activity against human RKOp27 cells after 48 hrs, EC50=0.09 μM
human HeLa cells	Cytotoxic assay	96 h	Cytotoxicity against human HeLa cells expressing telomerase after 96 hrs by MTT assay, IC50=0.1 μM
human SKOV3 cells	Proliferation assay	48 h	Antiproliferative activity against human SKOV3 cells after 48 hrs, EC50=0.12 μM
human NCI-H460 cells	Proliferation assay	48 h	Antiproliferative activity against human NCI-H460 cells after 48 hrs, EC50=0.12 μM
A549 cells	Cytotoxic assay		In vitro cytotoxic activity against human lung A549 cell line ( standard deviation in parenthesis), IC50=0.3 μM
SF268 cells	Proliferation assay	48 h	Antiproliferative activity against human SF268 cells after 48 hrs, EC50=0.32 μM
human KB/HeLa cells	Proliferation assay	48 h	Antiproliferative activity against human KB/HeLa cells after 48 hrs, EC50=0.36 μM
K562 cells	Growth inhibition assay	72 h	Growth inhibition of human K562 cells after 72 hrs by MTS method, IC50=0.42 μM
MDA-MB-231 cells	Proliferation assay		Antiproliferative activity against human MDA-MB-231 cells, IC50=0.96 μM
SF268 cells	Cytotoxic assay	48 h	Cytotoxicity against human SF268 cells after 48 hrs by SRB assay, GI50=0.97 μM
MDA435/LCC6 cells	Proliferation assay		Antiproliferative activity against multidrug resistant MDA435/LCC6 cells by ELISA, IC50=1.442 μM
U937 cells	Cytotoxic assay		Cytotoxicity against human U937 cells by MTT assay, IC50=6.2 μM
A549 cells	Cytotoxic assay		Cytotoxicity against human A549 cells by MTT assay, IC50=7.8 μM
HT-29 cell line	Proliferation assay		Inhibitory concentration of compound against proliferation of colon carcinoma HT-29 cell line, IC50=8 μM
HepG2 cells	Proliferation assay	48 h	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50=11.05 μM
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 88 mg/mL (197.98 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.100mg/ml (2.47mM)	Taking the 1 mL working solution as an example, add 50 μL of 22 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	444.48	Formula	C₂₂H₂₈N₄O₆	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	65271-80-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

Targets/IC₅₀/Ki	Topo II (Cell-free assay)
In vitro	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. This compound 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. It 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. This chemical induces apoptosis of PBMCs, monocytes and DCs at low concentrations, whereas higher doses causes cell lysis.
In vivo	Mitoxantrone transiently decreases the growth rate of HID xenografts in mice but does not affect that of PAC120 xenografts. This compound results in the severity of the cardiac lesions and the nephropathy and the intestinal toxicity in spontaneously hypertensive rats. This chemical and iron(III) form a strong 2:1 complex, in which it may be acting as a tridentate ligand.
References	[1] https://pubmed.ncbi.nlm.nih.gov/9450803/ [2] https://pubmed.ncbi.nlm.nih.gov/10940316/ [3] https://pubmed.ncbi.nlm.nih.gov/16171875/ [4] https://pubmed.ncbi.nlm.nih.gov/12686819/ [5] https://pubmed.ncbi.nlm.nih.gov/9299365/

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