Mitoxantrone

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

Mitoxantrone Chemical Structure

Mitoxantrone Chemical Structure

CAS No. 65271-80-9

Purity & Quality Control

Mitoxantrone Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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 9371240
human HL60 cells Cytotoxic assay 48 h Cytotoxicity against human HL60 cells after 48 hrs by MTT assay, GI50=0.33 nM 17962028
MDA435/LCC6 cells Proliferation assay Antiproliferative activity against MDA435/LCC6 cells by ELISA, IC50=0.35 nM 17154505
A2780-cell Growth inhibition assay Concentration required to inhibit A2780-cell growth by 50%, IC50=0.55 μM 9703471
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 9371240
G-361 cell Cytotoxic assay Cytotoxic potency required to inhibit G-361 cell growth by 50%, IC50=0.65 nM 9371240
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 10479282
human HL60 cells Proliferation assay 72 h Antiproliferative activity against human HL60 cells after 72 hrs by SRB assay, IC50=2.5 nM 22944121
human K562 cells Cytotoxic assay 5 days Cytotoxicity against human K562 cells after 5 days by XTT assay, IC50=2.6 nM 18076140
CH1-cell Growth inhibition assay Concentration required to inhibit CH1-cell growth by 50%, IC50=2.65 nM 9703471
uterine sarcoma MES-SA cells Cytotoxic assay In vitro cytotoxicity against uterine sarcoma MES-SA cells, IC5=3 nM 16169719
MES-SA cells Proliferation assay 72 h Antiproliferative activity against MES-SA cells by MTT assay after 72 hrs, IC50=3 nM 16824751
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 10956214
human LoVo cancer cell Cytotoxic assay 144 h Cytotoxicity against human LoVo cancer cell line was determined after 144 hr, IC50=3.3 nM 15456268
P388 cells Proliferation assay Antiproliferative activity against P388 cells by ELISA, IC50=4.3 nM 17154505
MCF-7 Growth inhibition assay In vitro inhibition of tumor cell growth in the human mammary tumor MCF-7 system, IC50=5 nM 1447730
murine L1210 sensitive cell line Function assay Anti-tumor activity against murine L1210 sensitive cell line by using MTT assay, IC50=5 nM 7699715
human Daudi cells Proliferation assay 72 h Antiproliferative activity against human Daudi cells after 72 hrs by MTT assay, IC50=5 nM 25998504
SKOV-3-cell Growth inhibition assay Concentration required to inhibit SKOV-3-cell growth by 50%, IC50=5.3 nM 9703471
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 10479282
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 15456268
OVCAR-3 cell Function assay Inhibitory activity against OVCAR-3 cell line, IC50=5.8 nM 8648600
human MES-SA cells Proliferation assay 72 h Antiproliferative activity against human MES-SA cells after 72 hrs by MTT assay, IC50=6 nM 25998504
human PC3 cancer cell Cytotoxic assay 144 h Cytotoxicity against human PC3 cancer cell line was determined after 144 hr, IC50=7 nM 15456268
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 10479282
WiDr cell Function assay Activity against human colon carcinoma sensitive WiDr cell line, IC50=8.1 nM 8960558
MXF7 breast cell line Function assay Antitumor activity against human mammary carcinoma sensitive MXF7 breast cell line, IC50=8.7 nM 8960558
HT-29 cell Cytotoxic assay In vitro cytotoxicity was tested against human colon adenocarcinoma HT-29 cell line, IC50=0.01 μM 10411474
CHO cell line xrs6 Cytotoxic assay Cytotoxicity against CHO cell line xrs6, IC50=0.01 μM 7473578
human HL60 cells Growth inhibition assay Growth inhibition of human HL60 cells by Almar blue assay, GI50=0.01 μM 17418582
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 15456268
human Ishikawa cells Proliferation assay 72 h Antiproliferative activity against human Ishikawa cells after 72 hrs by MTT assay, IC50=0.01 μM 25998504
HEK293 cells Cytotoxic assay 72 h Cytotoxicity against HEK293 cells after 72 hrs by MTT assay, IC50=0.01 μM 24611893
human MKN45 cancer cell Cytotoxic assay 144 h Cytotoxicity against human MKN45 cancer cell line was determined after 144 hr, IC50=0.012 μM 15456268
human LoVo cancer cell Cytotoxic assay 1 h Cytotoxicity against human LoVo cancer cell line was determined after 1 hr, IC50=0.012 μM 15456268
human FM3 cells Proliferation assay 72 h Antiproliferative activity against human FM3 cells after 72 hrs by MTT assay, IC50=0.013 μM 25998504
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 22582991
SK-BR-3 cells Function assay The IC50 value was measured on human breast cancer cell line SK-BR-3, IC50=0.016 μM 7699696
human small-cell lung cancer (SCLC) Cytotoxic assay Cytotoxicity against human small-cell lung cancer (SCLC), IC50=0.02 μM 8258835
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 21444205
human HCT116 cells Proliferation assay 72 h Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50=0.025 μM 25998504
A0375 cells Function assay Inhibitory activity against human tumor cell line A0375 melanoma, IC50=0.026 μM 7853345
NCI-H460 cells Cytotoxic assay 48 h Cytotoxicity against human NCI-H460 cells after 48 hrs by resazurin dye assay, EC50=0.03 μM 23988351
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 22582991
human HeLa cells Proliferation assay 72 h Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay, IC50=0.044 μM 25998504
human NCI60 cells Function assay 48 h Antitumor activity against human NCI60 cells after 48 hrs by SRB assay, GI50=0.04786 μM 18715786
UA375 cells Function assay Tested for inhibitory activity against human tumor cell line UA375 of melanoma using sulforhodamine B assay, IC50=0.048 μM 10956214
HT1080 cells Function assay Inhibitory activity against human tumor cell line HT1080, IC50=0.066 μM 7853345
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 25998504
human RKOp27 cells Proliferation assay 48 h Antiproliferative activity against human RKOp27 cells after 48 hrs, EC50=0.09 μM 23395656
human HeLa cells Cytotoxic assay 96 h Cytotoxicity against human HeLa cells expressing telomerase after 96 hrs by MTT assay, IC50=0.1 μM 18754611
human SKOV3 cells Proliferation assay 48 h Antiproliferative activity against human SKOV3 cells after 48 hrs, EC50=0.12 μM 23395656
human NCI-H460 cells Proliferation assay 48 h Antiproliferative activity against human NCI-H460 cells after 48 hrs, EC50=0.12 μM 23395656
A549 cells Cytotoxic assay In vitro cytotoxic activity against human lung A549 cell line ( standard deviation in parenthesis), IC50=0.3 μM 12036369
SF268 cells Proliferation assay 48 h Antiproliferative activity against human SF268 cells after 48 hrs, EC50=0.32 μM 23395656
human KB/HeLa cells Proliferation assay 48 h Antiproliferative activity against human KB/HeLa cells after 48 hrs, EC50=0.36 μM 23395656
K562 cells Growth inhibition assay 72 h Growth inhibition of human K562 cells after 72 hrs by MTS method, IC50=0.42 μM 18258442
MDA-MB-231 cells Proliferation assay Antiproliferative activity against human MDA-MB-231 cells, IC50=0.96 μM 18296053
SF268 cells Cytotoxic assay 48 h Cytotoxicity against human SF268 cells after 48 hrs by SRB assay, GI50=0.97 μM 17962028
MDA435/LCC6 cells Proliferation assay Antiproliferative activity against multidrug resistant MDA435/LCC6 cells by ELISA, IC50=1.442 μM 17154505
U937 cells Cytotoxic assay Cytotoxicity against human U937 cells by MTT assay, IC50=6.2 μM 19615900
A549 cells Cytotoxic assay Cytotoxicity against human A549 cells by MTT assay, IC50=7.8 μM 21458279
HT-29 cell line Proliferation assay Inhibitory concentration of compound against proliferation of colon carcinoma HT-29 cell line, IC50=8 μM 12031316
HepG2 cells Proliferation assay 48 h Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50=11.05 μM 24794747
Click to View More Cell Line Experimental Data

Biological Activity

Description Mitoxantrone is a type II topoisomerase inhibitor with IC50 of 2.0 μM, 0.42 mM for HepG2 and MCF-7/wt cells, respectively.
Targets
Topo II [1]
(Cell-free assay)
In vitro
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. [1] 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. [2] 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. [3]
In Vivo
In vivo Mitoxantrone transiently decreases the growth rate of HID xenografts in mice but does not affect that of PAC120 xenografts. [4] Mitoxantrone results in the severity of the cardiac lesions and the nephropathy and the intestinal toxicity in spontaneously hypertensive rats. Mitoxantrone and iron(III) form a strong 2:1 complex, in which mitoxantrone may be acting as a tridentate ligand. [5]

Chemical Information & Solubility

Molecular Weight 444.48 Formula

C22H28N4O6

CAS No. 65271-80-9 SDF Download Mitoxantrone SDF
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 88 mg/mL ( (197.98 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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