1. Cell Cycle/DNA Damage
  2. Topoisomerase
  3. Pixantrone

Pixantrone  (Synonyms: BBR 2778)

Cat. No.: HY-13727A Purity: 98.38%
COA Handling Instructions

Pixantrone (BBR 2778) dimaleate is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.

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

Pixantrone Chemical Structure

Pixantrone Chemical Structure

CAS No. : 144675-97-8

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 74 In-stock
Solution
10 mM * 1 mL in DMSO USD 74 In-stock
Solid
5 mg USD 60 In-stock
10 mg USD 90 In-stock
50 mg USD 280 In-stock
100 mg USD 420 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Pixantrone:

Top Publications Citing Use of Products

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Pixantrone (BBR 2778) dimaleate is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.

IC50 & Target[1]

Topoisomerase II

 

In Vitro

Pixantrone (0-10 μM, 72 h) dimaleate induces cell death in multiple cancer cell lines independent of cell cycle perturbation, with IC50s of 37.3 nM, 126 nM and 136 nM for T47D, MCF-10A and OVCAR5 cells, respectively[1].
? Pixantrone (25-500 nM, 2 4 h) dimaleate induces DNA damage at high concentration of 500 nM and induces severe chromosomal aberrations and mitotic catastrophe in PANC1 cells[1].
? Pixantrone (100 nM, 24 h) dimaleate may disrupt chromosome segregation because of generating merotelic kinetochore attachments that cause chromosome non-disjunction[1].
? Pixantrone (0-100 μM, 72 h) dimaleate potently inhibits growth of human leukemia K562 cells, etoposide-resistant K/VP.5 cells, MDCK and ABCB1-transfected MDCK/MDR cells with IC50s of 0.10 μM, 0.56 μM, 0.058 μM and 4.5 μM, respectively[2].
? Pixantrone (0.01-0.2 μM) dimaleate leads to a concentration-dependent formation of linear DNA through acting on topoisomerase Iiα and produces semiquinone free radicals in an enzymatic reducing system, although not in a cellular system, most likely due to low cellular uptake[2].
? Pixantrone (0.01-10 μM) dimaleate shows potent inhibitory activities against rat 97-116 peptide-specific T cell proliferation[4].

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

In Vivo

Pixantrone (i.v., 27 mg/kg, every 7 days, three times) dimaleate does not worsen pre-existing moderate degenerative cardiomyopathy, causes minimal cardiotoxic in mice following repeated treatment cycles and results in less mortality than Mitoxantrone (HY-13502) in Doxorubicin (HY-15142A)-pretreated mice[3].
? Pixantrone (i.v., 16.25 mg/kg, every week, three times) dimaleate modulates Lymph node cells (LNC) responses, affacts T cell subpopulations in TAChR-immunized Lewis rats and also shows preventive and therapeutic effect in experimental autoimmune myasthenia gravis (EAMG) rats[4].

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

Clinical Trial
Molecular Weight

557.51

Formula

C25H27N5O10

CAS No.
Appearance

Solid

Color

Blue to dark blue

SMILES

O=C(O)/C=C\C(O)=O.O=C(O)/C=C\C(O)=O.O=C(C1=C(NCCN)C=CC(NCCN)=C12)C3=C(C=NC=C3)C2=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (89.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 8.33 mg/mL (14.94 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7937 mL 8.9684 mL 17.9369 mL
5 mM 0.3587 mL 1.7937 mL 3.5874 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* 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
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 0.83 mg/mL (1.49 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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: ≥ 0.83 mg/mL (1.49 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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: 50 mg/mL (89.68 mM); Clear solution; Need ultrasonic

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.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.38%

References
Cell Assay
[1]

Briefly, cells seeded into 96-well plates are treated with increasing concentrations of either pixantrone or doxorubicin for 72 hours. After this time, MTS reagent is added to cells and incubated at 37°C for a further 4 hours. Cell proliferation is then determined by measuring the absorbance at 490 nm. All data points are normalized to untreated cells. All treatments are performed in triplicate and performed a minimum of 3 times[1].

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

Animal Administration
[3][4]

Mice[3]
To evaluate the potential cardiotoxicity of Pixantrone in doxorubicin-pretreated mice, doxorubicin 7.5 mg/kg is administered intravenously every 7 days for 3 weeks (1 cycle) to a group of CD1 females. Six weeks later, these mice receive either 0.9% saline (vehicle), doxorubicin 7.5 mg/kg, Pixantrone 27 mg/kg, or mitoxantrone 3 mg/kg intravenously every 7 days for 3 weeks (2 cycles). Animals are sacrificed after the first cycle at 8 weeks, and after the second cycle at 16 weeks. In addition, to evaluate the potential cardiotoxicity of Pixantrone as a single agent compared with doxorubicin and mitoxantrone, CD1 female mice receive a single or a double cycle of vehicle, doxorubicin 7.5 mg/kg, Pixantrone 27 mg/kg, or mitoxantrone 3 mg/kg. These animals are sacrificed after the first and second cycles (at 8 and 16 weeks, all groups), during week 14 (Pixantrone-treated group only) and during week 22 (Pixantrone- and vehicle-treated groups)[3].
Rats[4]
For the studies on Pixantrone efficacy on EAMG, TAChR-immunized rats are randomly assigned to different treatment groups: 1) preventive Pixantrone group, starting 4 days after immunization, with 16.25 mg/kg Pixantrone, administered i.v. via tail vein, once a week for three times; 2) therapeutic Pixantrone group, starting 4 wk after immunization, with 16.25 mg/kg Pixantrone, administered i.v. via tail vein, once a week for three times; 3) therapeutic MTX group (1.2 mg/kg, i.v. via tail vein, once a week for three times); and 4) vehicle group (sterile saline, i.v. via tail vein, once a week for three times). The doses of Pixantrone and MTX used in this study are in both cases equal to one-fourth of the LD10 for single i.v. injection in rats. Treatment assignation is performed at day 4 after TAChR immunization (preventive schedule) in coincidence of the acute phase of EAMG, or at onset of clinical signs (therapeutic schedule), which occurs after 4 wk. Animals are sacrificed after deep anesthesia obtained by carbon dioxide; low-grade anesthesia with chloral hydrate administered i.p. is used for TAChR immunization and drug treatments[4].

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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.7937 mL 8.9684 mL 17.9369 mL 44.8422 mL
5 mM 0.3587 mL 1.7937 mL 3.5874 mL 8.9684 mL
10 mM 0.1794 mL 0.8968 mL 1.7937 mL 4.4842 mL
DMSO 15 mM 0.1196 mL 0.5979 mL 1.1958 mL 2.9895 mL
20 mM 0.0897 mL 0.4484 mL 0.8968 mL 2.2421 mL
25 mM 0.0717 mL 0.3587 mL 0.7175 mL 1.7937 mL
30 mM 0.0598 mL 0.2989 mL 0.5979 mL 1.4947 mL
40 mM 0.0448 mL 0.2242 mL 0.4484 mL 1.1211 mL
50 mM 0.0359 mL 0.1794 mL 0.3587 mL 0.8968 mL
60 mM 0.0299 mL 0.1495 mL 0.2989 mL 0.7474 mL
80 mM 0.0224 mL 0.1121 mL 0.2242 mL 0.5605 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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Pixantrone Related Classifications

Help & FAQs
  • 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.

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