Home DNA Damage/DNA Repair Topoisomerase inhibitor - COVID-19 inhibitor - Apoptosis related activator - PKC inhibitor Mitoxantrone 2HCl For research use only.

Mitoxantrone 2HCl

Synonyms: NSC-301739 2HCl, Mitozantrone 2HCl

Mitoxantrone 2HCl is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor of type II topoisomerase and protein kinase C (PKC) with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 of 0.42 μM. Mitoxantrone also induces apoptosis.

Mitoxantrone 2HCl Chemical Structure

Mitoxantrone 2HCl Chemical Structure

CAS No. 70476-82-3

Purity & Quality Control

Mitoxantrone 2HCl Related Products

Signaling Pathway

Topoisomerase Signaling Pathways

Topoisomerase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
L1210 cell Cytotoxicity 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
HL60 cells Cytotoxicity assay 48 h Cytotoxicity against human HL60 cells after 48 hrs by MTT assay, GI50=0.33 μM 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 nM 9703471
G-361 cell Growth inhibition assay Cytotoxic potency required to inhibit G-361 cell growth by 50%, IC50=0.65 nM 9371240
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 Cytotoxicity assay 5 days Cytotoxicity against human K562 cells after 5 days by XTT assay, IC50=2.6 nM 18076140
CH1 cell Cytotoxicity assay Cytotoxic potency required to inhibit CH1 cell growth by 50%, IC50=2.65 nM 9371240
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 Activity against A549 cancer cell line, IC50=3.1 nM 8960558
LoVo cells Cytotoxicity 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
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 Cytotoxicity assay Cytotoxic potency required to inhibit SKOV-3 cell growth 50%, IC50=5.3 nM 9371240
OVCAR-3 cell Function assay Antitumor activity against human ovarian OVCAR-3 cell lines, IC50=5.8 nM 8960558
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
PC3 cancer cell Cytotoxicity assay 144 h Cytotoxicity against human PC3 cancer cell line was determined after 144 hr, IC50=7 nM 15456268
MXF7 breast cell Function assay Antitumor activity against human mammary carcinoma sensitive MXF7 breast cell line, IC50=8.7 nM 8960558
HT-29 cell Cytotoxicity assay 144 h Cytotoxic potency required to inhibit HT-29 cell growth by 50% after cell drug contact for 144 hrs, IC5=0.01 μM 9371240
HEK293 cells Cytotoxicity assay 72 h Cytotoxicity against HEK293 cells after 72 hrs by MTT assay, IC50=0.01 μM 24611893
MKN45 cells Cytotoxicity assay 144 h Cytotoxicity against human MKN45 cancer cell line was determined after 144 hr, IC50=0.012 μM 15456268
MES-SA cells Cytotoxicity assay 72 h Cytotoxicity against human MES-SA cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50=0.012 μM 21444205
FM3 cells Proliferation assay 72 h Antiproliferative activity against human FM3 cells after 72 hrs by MTT assay, IC50=0.013 μM 25998504
MCF-7 cells Growth inhibition assay Inhibitory activity against human tumor cell line MCF-7 breast adenocarcinoma, IC50=0.02 μM 7853345
human small-cell lung cancer Cytotoxicity assay Cytotoxicity against human small-cell lung cancer (SCLC), IC50=0.02 μM 8258835
human HCT116 cells Cytotoxicity 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
NCI-H460 cells Cytotoxicity assay 48 h Cytotoxicity against human NCI-H460 cells after 48 hrs by resazurin dye assay, EC50=0.03 μM 23988351
CCRF-CEM cells Cytotoxicity 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
HeLa cells Proliferation assay 72 h Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay, IC50=0.044 μM 25998504
NCI60 cells Function assay 48 h Antitumor activity against human NCI60 cells after 48 hrs by SRB assay, GI50=47.86 nM 18715786
UACC375 cell Function assay Antitumor activity against human melanoma UACC375 cell line, IC50=0.048 μM 8960558
HT1080 cell Growth inhibition assay Inhibitory activity against human tumor cell line HT1080, IC50=0.066 μM 7853345
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
SF268 cells Proliferation assay 48 h Antiproliferative activity against human SF268 cells after 48 hrs, EC50=0.32 μM 23395656
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 72 h Antiproliferative activity against human MDA-MB-231 cells by WST-1 method after 72 hrs, IC50=0.96 μM 17335189
SF268 cells Cytotoxicity assay 48 h Cytotoxicity against human SF268 cells after 48 hrs by SRB assay, GI50=0.97 μM 17962028
HCT116 cells Cytotoxicity assay Cytotoxicity against human HCT116 cells by MTT assay, IC50=3.96 μM 20951582
U937 cells Cytotoxicity assay Cytotoxicity against human U937 cells by MTT assay, IC50=6.2 μM 19615900
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 2HCl is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor of type II topoisomerase and protein kinase C (PKC) with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 of 0.42 μM. Mitoxantrone also induces apoptosis.
Targets
Topoisomerase II [1] PKC [7]
(Cell-free assay)
8.5 μM
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]
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-ROS1 / ROS1 / p-STAT3 / STAT3 / p-AKT / AKT / p-ERK / ERK 30108778
Growth inhibition assay Cell number 24349321
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06156761 Not yet recruiting
Breast Cancer
Cancer Institute and Hospital Chinese Academy of Medical Sciences|CSPC Ouyi Pharmaceutical Co. Ltd.
 November 28 2023 Not Applicable
NCT05875428 Recruiting
Diffuse Large B-Cell Lymphoma
CSPC ZhongQi Pharmaceutical Technology Co. Ltd.
 July 10 2023 Phase 2
NCT05496894 Withdrawn
Relapsing Multiple Sclerosis
CSPC Zhongnuo Pharmaceutical (Shijiazhuang) Co. Ltd.
 August 2022 Phase 2

Chemical Information & Solubility

Molecular Weight 517.4 Formula

C22H29ClN4O6.2HCl
CAS No. 70476-82-3 SDF Download Mitoxantrone 2HCl SDF
Smiles C1=CC(=C2C(=C1NCCNCCO)C(=O)C3=C(C=CC(=C3C2=O)O)O)NCCNCCO.Cl.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 104 mg/mL ( (201.0 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 104 mg/mL

Ethanol : Insoluble


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In vivo
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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. )

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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.

Handling Instructions

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