2. Cell Cycle/DNA Damage
  3. Topoisomerase
  4. Banoxantrone dihydrochloride

Banoxantrone dihydrochloride  (Synonyms: AQ4N dihydrochloride)

Cat. No.: HY-13562A Purity: 99.46%
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Banoxantrone dihydrochloride is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.

For research use only. We do not sell to patients.

Banoxantrone dihydrochloride Chemical Structure

Banoxantrone dihydrochloride Chemical Structure

CAS No. : 252979-56-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Solution
10 mM * 1 mL in DMSO USD 109 In-stock
Solid
5 mg USD 96 In-stock
10 mg USD 168 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Banoxantrone dihydrochloride:

Banoxantrone dihydrochloride Related Antibodies

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Topoisomerase Topo I Topo II

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Banoxantrone dihydrochloride is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.

IC50 & Target[1]

Topoisomerase II

 

In Vitro

Banoxantrone (AQ4N) can be reduced in a hypoxic environment to a stable DNA-affinic agent AQ4. AQ4, a potent topoisomerase II inhibitor, would be capable of damaging cells recruited into the cell cycle following radiation damage to the well-oxygenated cells of the tumor[1]. Banoxantrone shows more than 8-fold higher cytotoxicity under hypoxia than normoxia in cultures of 9L rat gliosarcoma and H460 human non-small-cell lung carcinoma cells but not for 11 other human cancer cell lines. DT-diaphorase protein levels and banoxantrone chemosensitivity are poorly correlated across the cancer cell line panel, and banoxantrone chemosensitivity is not affected by DT-diaphorase inhibitors[2]. Banoxantrone is a bis-N-oxide that is reduced via two sequential two-electron reductions to the tertiary amine, AQ4, which is a potent cytotoxic agent toward both aerobic and hypoxic cells. AQ4, but not AQ4N, intercalates in DNA with high affinity to generate a stable persistent complex that can inhibit topoisomerase II and cause DNA damage and cell death[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Banoxantrone dihydrochloride Related Antibodies
In Vivo

Banoxantrone (200 mg/kg) significantly enhances the tumor growth delay caused by radiation. This occurred when radiation is administered both as a single dose (12 Gy) and in a multifraction regimen (5x3 Gy). A study of the scheduling of Banoxantrone (AQ4N) administration shows that there is a very long time period over which a maximal effect can be elicited (drug given 4 days before to 6 h after radiation). These results suggest that Banoxantrone has significant potential as a bioreductive drug[1]. The activation of banoxantrone cytotoxicity in vivo requires tumor hypoxia that is more extensive or prolonged than can readily be achieved by vasodilation or by antiangiogenic drug treatment[2]. Incorporation of banoxantrone into conventional chemoradiation protocols therefore targets both oxygenated and hypoxic regions of tumors, and potentially will increase the effectiveness of therapy. A single dose of 60 mg/kg banoxantrone enhances the response of RT112 (bladder) and Calu-6 (lung) xenografts to treatment with cisplatin and radiation therapy. Banoxantrone will increase the efficacy of chemoradiotherapy in preclinical models[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

517.40

Formula

C22H30Cl2N4O6
CAS No.
Appearance

Solid

Color

Blue to dark blue

SMILES

O=C1C2=C(C(O)=CC=C2O)C(C3=C(NCC[N+](C)(C)[O-])C=CC(NCC[N+](C)(C)[O-])=C13)=O.Cl.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 2 years; -20°C, 1 year (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (48.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 20 mg/mL (38.65 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9327 mL 9.6637 mL 19.3274 mL
5 mM 0.3865 mL 1.9327 mL 3.8655 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light, stored under nitrogen). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 7.5 mg/mL (14.50 mM); Clear solution

    This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 7.5 mg/mL (14.50 mM); Clear solution

    This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 8.33 mg/mL (16.10 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.46%

SDS (419 KB)

COA (253 KB) HNMR (383 KB) LCMS (99 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

Untreated T50/80 tumors (6.5-9.0 mm geometric diameter (GMD) are excised and gently disaggregated by mechanical disruption in ice-cold phosphate-buffered saline (PBS). Single cell suspensions are prepared by filtration through a 40μm mesh. These are then centrifuged and resuspended in Eagle's minimal essential medium (EMEM) containing 10% fetal calf serum (FCS) at a concentration of 106 cells/mL. Cells (20 mL) are placed in 125 mL rubber sealed glass bottles. These are gassed for 2 h at 37°C to provide welloxygenated conditions, i.e. 95% air/5% carbon dioxide or hypoxic conditions 95% N2/5% CO2. Banoxantrone (AQ4N) (20μM) is added for the last 90 min of this period by injection through the sealed lid. Drug is washed off and cells resuspended in fresh medium. For analysis of DNA damage, aliquots (105 cells) are processed at various times ranging from 0 to 96 h after this procedure. To evaluate the effect of maintaining the excised tumor cells in culture, samples are also maintained in the culture medium above at 37°C, 95% air/5% CO2 for 24 h. The cells, which grow in suspension, are then harvested and placed in glass bottles and the experiment outlined above is carried out. Each experiment is carried out twice and the results pooled[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
T50/80 tumor-bearing mice are used. These experiments are carried out when tumors reach a geometric diameter (GMD) of 6.5-9.0 mm. Banoxantrone (AQ4N) is administered as a single i.p. injection at a dose of 200 mg/kg. The drug is given 30 min before a single dose of X-irradiation of 12 Gy (300 kVp Siemens Stabilipan with a dose rate of 2.56 Gy min-1). Tumors are excised at a range of times following treatment and placed on ice. Single cell suspensions are prepared in ice-cold PBS as outlined above. Following centrifugation the cells are diluted in cold EMEM containing 10% FCS (1x106 cells/mL). An aliquot of 100 μL of this suspension is used in the comet assay. This procedure is carried out on tumors excised at various time intervals ranging from 0 to 120 h following irradiation. The results are pooled from three individual experiments.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light, stored under nitrogen). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.9327 mL 9.6637 mL 19.3274 mL 48.3185 mL
5 mM 0.3865 mL 1.9327 mL 3.8655 mL 9.6637 mL
10 mM 0.1933 mL 0.9664 mL 1.9327 mL 4.8319 mL
15 mM 0.1288 mL 0.6442 mL 1.2885 mL 3.2212 mL
20 mM 0.0966 mL 0.4832 mL 0.9664 mL 2.4159 mL
25 mM 0.0773 mL 0.3865 mL 0.7731 mL 1.9327 mL
30 mM 0.0644 mL 0.3221 mL 0.6442 mL 1.6106 mL
DMSO 40 mM 0.0483 mL 0.2416 mL 0.4832 mL 1.2080 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Banoxantrone dihydrochloride Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Banoxantrone252979-56-9AQ4NTopoisomeraseInhibitorinhibitorinhibit

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