Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
1g |
|
||
Other Sizes |
|
Pixantrone dimaleate, the dimaleate salt of Pixantrone (formerly known as BBR 2778) and an aza-anthracenedione analog, is a weak topoisomerase II inhibitor and DNA intercalator with anticancer activity with little cardiotoxicity. It interacts by alkylating specific DNA hypermethylated sites to form stable DNA adducts.
Targets |
Topoisomerase II
|
||
---|---|---|---|
ln Vitro |
|
||
ln Vivo |
|
||
Cell Assay |
Pixantrone or doxorubicin at escalating concentrations is applied to cells seeded into 96-well plates for a duration of 72 hours. Subsequently, the cells are treated with MTS reagent and given a 4-hour incubation period at 37°C. Finally, the absorbance at 490 nm is measured to estimate cell proliferation. For every data point, untreated cells are used as a normal. Every therapy is administered three times at the very least in triplicate.
|
||
Animal Protocol |
|
||
References |
|
||
Additional Infomation |
Pixantrone Dimaleate is the dimaleate salt of a synthetic, noncardiotoxic aza-anthracenedione analogue with potential antineoplastic activity. Pixantrone intercalates into DNA and induces topoisomerase II-mediated DNA strand crosslinks, resulting in inhibition of DNA replication and tumor cell cytotoxicity.
Drug Indication Pixuvri is indicated as monotherapy for the treatment of adult patients with multiply relapsed or refractory aggressive non-Hodgkin B-cell lymphomas (NHL). The benefit of pixantrone treatment has not been established in patients when used as fifth-line or greater chemotherapy in patients who are refractory to last therapy. Treatment of non-Hodgkin lymphoma |
Molecular Formula |
C17H19N5O2.2C4H4O4
|
|
---|---|---|
Molecular Weight |
557.51
|
|
Exact Mass |
557.18
|
|
Elemental Analysis |
C, 53.86; H, 4.88; N, 12.56; O, 28.70
|
|
CAS # |
144675-97-8
|
|
Related CAS # |
144510-96-3; 175989-38-5 (HCl); 144675-97-8
|
|
PubChem CID |
9937618
|
|
Appearance |
Brown to black solid powder
|
|
Boiling Point |
650ºC at 760mmHg
|
|
Flash Point |
346.9ºC
|
|
Vapour Pressure |
8.89E-17mmHg at 25°C
|
|
LogP |
1.856
|
|
Hydrogen Bond Donor Count |
8
|
|
Hydrogen Bond Acceptor Count |
15
|
|
Rotatable Bond Count |
10
|
|
Heavy Atom Count |
40
|
|
Complexity |
591
|
|
Defined Atom Stereocenter Count |
0
|
|
SMILES |
O=C1C2C([H])=C([H])N=C([H])C=2C(C2=C(C([H])=C([H])C(=C21)N([H])C([H])([H])C([H])([H])N([H])[H])N([H])C([H])([H])C([H])([H])N([H])[H])=O.O([H])C(/C(/[H])=C(\[H])/C(=O)O[H])=O
|
|
InChi Key |
SVAGFBGXEWPNJC-SPIKMXEPSA-N
|
|
InChi Code |
InChI=1S/C17H19N5O2.2C4H4O4/c18-4-7-21-12-1-2-13(22-8-5-19)15-14(12)16(23)10-3-6-20-9-11(10)17(15)24;2*5-3(6)1-2-4(7)8/h1-3,6,9,21-22H,4-5,7-8,18-19H2;2*1-2H,(H,5,6)(H,7,8)/b;2*2-1-
|
|
Chemical Name |
6,9-bis(2-aminoethylamino)benzo[g]isoquinoline-5,10-dione;(Z)-but-2-enedioic acid
|
|
Synonyms |
|
|
HS Tariff Code |
2934.99.9001
|
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
|
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
|
|||
---|---|---|---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (1.49 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.83 mg/mL (1.49 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 50 mg/mL (89.68 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 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 | |
10 mM | 0.1794 mL | 0.8968 mL | 1.7937 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT01086605 | Completed | Drug: pixantrone dimaleate | Breast Cancer | Alliance for Clinical Trials in Oncology |
May 2010 | Phase 2 |
NCT01321541 | Completed | Drug: Pixantrone + Rituximab Drug: Gemcitabine + Rituximab |
Follicular Grade 3 Lymphoma de Novo DLBCL |
CTI BioPharma | April 20, 2011 | Phase 3 |
Comparison of the preventive and therapeutic PIX treatments on EAMG manifestation.J Immunol.2008 Feb 15;180(4):2696-703. th> |
---|
Variations in clinical score and body weight in EAMG rats.J Immunol.2008 Feb 15;180(4):2696-703. td> |
Immunological evaluation of the therapeutic PIX and MTX treatments in EAMG rats.J Immunol.2008 Feb 15;180(4):2696-703. td> |