Fig. 1 · Structure

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Mitoxantrone

Mitoxantrone is a synthetic antineoplastic anthracenedione (IC50 = 0.42 mM).

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Biological Activity

Target & Activity

Target Activity Value
Topo II (Cell-free assay)

Cellular Effect

Cell Line Activity Value Description Reference
2008 IC50 7.8 nM Antiproliferative activity against human 2008 cells assessed as reduction in cell viability after 5 days by MTS/PMS assay [PMID: 31465686]
A2780 IC50 0.00055 μM Concentration required to inhibit A2780-cell growth by 50% [PMID: 9703471]
A2780 IC50 0.00055 μM Cytotoxic potency required to inhibit A2780 cell growth by 50% after cell drug contact for 96 hrs [PMID: 9371240]
A-375 IC50 111.5 nM Cytotoxicity against human A375 cells assessed as reduction in cell viability preincubated for 5 hrs followed by compound washout and measured after 48 hrs by CCK8 assay [PMID: 30925340]
A549 IC50 0.036 nM Antiproliferative activity against human A549 cells after 72 hrs by sulforhodamine B assay [PMID: 30485090]
A549 IC50 15.7 μg/mL Cytotoxicity against human A549 cells after 24 hrs by MTT assay [PMID: 26599534]
A549 IC50 25.3 μg/mL Cytotoxicity against Homo sapiens (human) A549 cells after 24 hr by MTT assay 10.1007/s00044-012-0325-2
A549 IC50 3 nM 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. [PMID: 10956214]
A549 IC50 7.25 μM Cytotoxicity against human A549 cells after 48 hrs by MTT assay [PMID: 30684866]
A549 IC50 7.8 μM Cytotoxicity against human A549 cells after 24 hrs by MTT assay [PMID: 21507644]
A549 IC50 7.8 μM Cytotoxicity against human A549 cells by MTT assay [PMID: 21458279]
A549 IC50 7.83 μM Cytotoxicity against human A549 cells after 72 hrs [PMID: 21354791]
A549 IC50 8 μM Cytotoxicity against human A549 cells by MTT assay [PMID: 19615900]
A549 GI50 8.3 μM Growth inhibition of human A549 cells by MTT assay [PMID: 20153184]
Bel-7402 IC50 116.6 nM Cytotoxicity against human Bel7402 cells assessed as reduction in cell viability preincubated for 5 hrs followed by compound washout and measured after 48 hrs by CCK8 assay [PMID: 30925340]
C6 IC50 10.9 μg/mL Cytotoxicity against Rattus norvegicus (rat) C6 cells after 24 hr by MTT assay 10.1007/s00044-012-0325-2
C6 IC50 11 μg/mL Cytotoxicity against rat C6 cells after 24 hrs by MTT assay [PMID: 26599534]
Caco-2 IC50 > 10 μM Cytotoxicity against NAE-knockdown human Caco2 cells after 72 hrs by MTT assay [PMID: 29232579]
Caco-2 IC50 1.4 μM Cytotoxicity against human Caco2 cells after 72 hrs by MTT assay [PMID: 29232579]
Cancer cell lines IC50 0.75 nM Cytotoxicity against human H460M cancer cell line was determined after 144 hr [PMID: 15456268]

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In Vitro Studies

In HEK293T cells treated at 5 µM for 6 h, differential gene expression analyses reported that Mitoxantrone had the most significant impact on gene expression. In MCF-7 cells exposed for 72 hr, Mitoxantrone increased lysosome number per cell 2.7-fold at sub-cytotoxic concentrations as low as 10 nM and 3.9-fold at 30 nM. Mitoxantrone exposure at 30 nM for 72 hr also increased mean lysosome size, measured as cross-sectional lysosomal area, 1.9-fold in MCF-7 cells. In HEK-293 cells transfected with empty vector, Mitoxantrone treatment for 96 h yielded a reported IC50 of 3.8±1.8 nM. [1,2,3]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Mitoxantrone Effects on Gene Expression

Cell-based study · HEK293T cells [1]

HEK293T cells were treated with Mitoxantrone at 5 µM for 6 h, with untreated HEK293T cells as controls. Differential gene expression analyses reported that Mitoxantrone had the most significant impact on gene expression.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Differential gene expression analysesReported result Mitoxantrone had the most significant impact on gene expression[1]

Literature-Reported Treatment Conditions

Treatment concentration
5 µM
Exposure duration
for 6 h
Reported limits
Not stated in the sentences used: route, vehicle.
Methods and source locations

Compound reported in the paper: Mitoxantrone

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Results > A combination regimen optimally targeting the HS-assisted viral entry (S135, S136, S138); Materials and methods > qRT-PCR analysis of knockout or knockdown cells (S231, S232)

Differential gene expression analyses: Differential gene expression analyses; comparator: untreated HEK293T cells — Results > A combination regimen optimally targeting the HS-assisted viral entry (S136)

Mitoxantrone Exposure and Lysosome Number

Cell-based study · MCF-7 cells [2]

MCF-7 cells were exposed to Mitoxantrone for 72 hr. Lysosome number per cell increased 2.7-fold at sub-cytotoxic concentrations as low as 10 nM and 3.9-fold at 30 nM.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Lysosome numberlysosome number per cell 2.7-fold increase; 3.9-fold increase[2]

Literature-Reported Treatment Conditions

Treatment concentration
1–100 nM
Exposure duration
72 hr
Method
exposed
Reported limits
Not stated in the sentences used: vehicle, control.
Methods and source locations

Compound reported in the paper: Mitoxantrone

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

RESULTS > Exposure of MCF-7 cells to hydrophobic weak base drugs induces an increase in lysosome number (S24, S25); Figure 3 legend (S97, S98, S99)

Lysosome number: Lysosome number — RESULTS > Exposure of MCF-7 cells to hydrophobic weak base drugs induces an increase in lysosome number (S24, S25); Figure 3 legend (S99)

Mitoxantrone Response in Empty Vector Transfected Cells

Cell-based study · HEK-293 cells transfected with empty vector [3]

HEK-293 cells transfected with empty vector received various concentrations of Mitoxantrone for 96 h. The reported IC50 was 3.8±1.8 nM.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
IC50 (nM)IC50 3.8±1.8 nM[3]

Literature-Reported Treatment Conditions

Treatment concentration
various concentrations
Exposure duration
96 h at 37°C in 5% CO2
Method
added to the cells
Reported limits
Not stated in the sentences used: vehicle, control.
Methods and source locations

Compound reported in the paper: Mitoxantrone

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

MATERIALS AND METHODS > Cytotoxicity assays (S29, S30); Figure 3 legend (S123); Table 2 (T2.h1, T2.h2, T2.r1)

IC50 (nM): IC50 (nM) — Table 2 (T2.h1, T2.h2, T2.r1)

Mitoxantrone Exposure and Mean Lysosome Size

Cell-based study · MCF-7 cells [2]

MCF-7 cells were exposed to Mitoxantrone at 30 nM for 72 hr. Mean lysosome size, determined as cross-sectional lysosomal area, increased 1.9-fold.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
mean size of lysosomes (determined as the cross-sectional lysosomal area)mean size of lysosomes 1.9-fold increase[2]

Literature-Reported Treatment Conditions

Treatment concentration
30 nM
Exposure duration
72 hr
Method
exposed
Reported limits
Not stated in the sentences used: vehicle, control.
Methods and source locations

Compound reported in the paper: Mitoxantrone

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

RESULTS > Exposure of MCF-7 cells to hydrophobic weak base drugs induces an increase in lysosome number (S22, S25)

mean size of lysosomes (determined as the cross-sectional lysosomal area): mean size of lysosomes (determined as the cross-sectional lysosomal area) — RESULTS > Exposure of MCF-7 cells to hydrophobic weak base drugs induces an increase in lysosome number (S25)

Specifications

Manufacturer Adooq Bioscience
CAS Number 65271-80-9
Formula C22H28N4O6
Molecular Weight 444.5
SMILES
C1=CC(=C2C(=C1NCCNCCO)C(=O)C3=C(C=CC(=C3C2=O)O)O)NCCNCCO

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Zhang Q, Chen CZ, Swaroop M, et al. Heparan sulfate assists SARS-CoV-2 in cell entry and can be targeted by approved drugs in vitro. Cell Discov (2020). PMID: 33298900 DOI: 10.1038/s41421-020-00222-5 Source material
  2. [2] Zhitomirsky B, Assaraf YG. Lysosomal sequestration of hydrophobic weak base chemotherapeutics triggers lysosomal biogenesis and lysosome-dependent cancer multidrug resistance. Oncotarget (2015). PMID: 25544758 DOI: 10.18632/oncotarget.2732 Source material
  3. [3] Robey RW, Honjo Y, Morisaki K, et al. Mutations at amino-acid 482 in the ABCG2 gene affect substrate and antagonist specificity. Br J Cancer (2003). PMID: 14612912 DOI: 10.1038/sj.bjc.6601370 Source material

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