Pixantrone free base
Based on 3 publication(s) in Google Scholar
Pixantrone (BBR 2778 (free base)), a mitoxantrone analog, is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
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- CAS. Nr.: 144510-96-3
- Formel: C17H19N5O2
- Molecular Weight:325.37
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Pixantrone free base
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Biologische Aktivität
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Topoisomerase II |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-29 | GI50 |
0.0012 μM
Compound: pix, pixantrone
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Cytotoxicity against human HT29 cells after 72 hrs
Cytotoxicity against human HT29 cells after 72 hrs
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[PMID: 18232651] |
| LoVo | IC50 |
0.24 μg/mL
Compound: 3e
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Tested in vitro for cytotoxic activity against Human colon Adenocarcinoma sensitive cell line (LoVo)
Tested in vitro for cytotoxic activity against Human colon Adenocarcinoma sensitive cell line (LoVo)
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[PMID: 8145234] |
| LoVo | IC50 |
7.2 μg/mL
Compound: 3e
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Tested in vitro for cytotoxic activity against Doxorubicin resistant Human colon Adenocarcinoma sensitive cell line
Tested in vitro for cytotoxic activity against Doxorubicin resistant Human colon Adenocarcinoma sensitive cell line
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[PMID: 8145234] |
Pixantrone (0-10 μM, 72 h) induces cell death in multiple cancer cell lines independent of cell cycle perturbation[1].
Pixantrone (25-500 nM, 24 h) can induce DNA damage, hinder chromosome segregation, and induce severe chromosomal aberrations and mitotic catastrophes in PANC1 cells[1].
Pixantrone (0-100 μM, 72 h) 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) 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) 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.
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Cell Line:T47D, MCF-10A and OVCAR5 cells
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Concentration:0-10 μM
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Incubation Time:72 h
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Result:Reduced the proliferation of T47D, MCF-10A and OVCAR5 cells with 37.3 nM, 126 nM and 136 nM, respectively.
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Cell Line:Lewis rat T cell lines
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Concentration:0.01-10 μM
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Incubation Time:
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Result:Inhibited 39.3% rat 97-116 peptide-specific T cells proliferation at 0.01 μM and completely suppressed T cell proliferation at high concentrations.
Pixantrone (i.v., 16.25 mg/kg, every week, three times) 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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 144510-96-3
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Molecular Weight 325.37
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Formel C17H19N5O2
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SMILES
O=C(C1=C(NCCN)C=CC(NCCN)=C12)C3=C(C=NC=C3)C2=O
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Synonyms
BBR 2778 free base
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
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Journal Impact Factor
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Most Recent
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Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
Methods Mol Biol
2018:1711:351-398. PMID: 29344898
Reinheit & Dokumentation
Verweise
[1]. Beeharry N, et al. Pixantrone induces cell death through mitotic perturbations and subsequent aberrant cell divisions. Cancer Biol Ther. 2015;16(9):1397-406. [Content Brief]
[2]. Hasinoff BB, et al. Mechanisms of Action and Reduced Cardiotoxicity of Pixantrone; a Topoisomerase II Targeting Agent with Cellular Selectivity for the Topoisomerase IIα Isoform. J Pharmacol Exp Ther. 2016 Feb;356(2):397-409. [Content Brief]
[3]. Cavalletti E, et al. Pixantrone (BBR 2778) has reduced cardiotoxic potential in mice pretreated with doxorubicin: comparative studies against doxorubicin and mitoxantrone. Invest New Drugs. 2007 Jun;25(3):187-95. [Content Brief]
[4]. Ubiali F, et al. Pixantrone (BBR2778) reduces the severity of experimental autoimmune myasthenia gravis in Lewis rats. J Immunol. 2008 Feb 15;180(4):2696-703. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Pixantrone free base Related Classifications
HY-13727 Related Classifications
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