Pixantrone maleate
Benz(g)isoquinoline-5,10-dione, 6,9-bis((2-aminoethyl)amino)-, (2Z)-2- butenedioate (1:2)
CAS: 144675-97-8
Molecular Formula: C21H23N5O6
Pixantrone maleate - Names and Identifiers
| Name | Benz(g)isoquinoline-5,10-dione, 6,9-bis((2-aminoethyl)amino)-, (2Z)-2- butenedioate (1:2) |
| Synonyms | CS-1295 Pixolti Pixuvri BBR 2778 Bbr 2778 UNII-P0R64C4CR9 Pixantrone maleate BBR 2778 dimaleate Pixatrone dimaleate Pixantrone-dimaleate, BBR2778 dimaleate 6,9-bis[(2-aminoethyl)amino]benzo[g]isoquinoline-5,10-dione di[(2E)-but-2-enedioate] |
| CAS | 144675-97-8 |
| EINECS | 680-661-5 |
| InChI | InChI=1/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+ |
Pixantrone maleate - Physico-chemical Properties
| Molecular Formula | C21H23N5O6 |
| Molar Mass | 441.43722 |
| Melting Point | 192° |
| Boling Point | 650°C at 760 mmHg |
| Flash Point | 346.9°C |
| Solubility | DMSO : 33.33 mg/mL (59.78 mM; Need ultrasonic)H2O : 16.67 mg/mL (29.90 mM; Need ultrasonic) |
| Vapor Presure | 8.89E-17mmHg at 25°C |
| Storage Condition | under inert gas (nitrogen or Argon) at 2-8°C |
| Use | Pixantrone dimaleate is an inhibitor of topoisomerase II (topoisomerase II) and DNA intercalation agent with antitumor activity. |
| In vitro study | Pixantrone dimaleate is a topoisomerase II inhibitor. Pixantrone induces cell death in multiple cancer cell lines independent of cell cycle perturbation, with IC 50 s of 37.3 nM, 126 nM and 136 nM for T47D, MCF-10A and OVCAR5 cells, respectively. Pixantrone induces DNA damage at high concentrations (500 nM) but not at concentrations (100 nM) sufficient to kill PANC1 cells. Pixantrone (25 or 100 nM) induces severe chromosomal aberrations and mitotic catastrophe in PANC1 cells. Pixantrone (100 nM) may disrupt chromosome segregation because of generating merotelic kinetochore attachments that cause chromosome non-disjunction. Pixantrone potently inhibits growth of human Leukemia K562 cells, etoposide-resistant K/VP.5 cells, MDCK and ABCB1-transfected MDCK/MDR cells, with IC 50 s of 0.10 μM, 0.56 μM, 0.058 μM and 4.5 μM, respectively. Pixantrone (0.01-0.2 μM) leads to a concentration-dependent formation of linear DNA through acting on topoisomerase IIα. Pixantrone produces semiquinone free radicals in an enzymatic reducing system, although not in a cellular system, most likely due to low cellular uptake. Pixantrone (0.01-10 μM) shows potent inhibitory activities against rat 97-116 peptide-specific T cell proliferation. |
| In vivo study | Pixantrone (27 mg/kg) does not worsen pre-existing moderate degenerative cardiomyopathy in doxorubicin-pretreated mice, by i.v. one dose every 7 days repeated thrice (q7d × 3). Pixantrone (27 mg/kg) causes minimal cardiotoxic in mice following repeated treatment cycles. Moreover, Pixantrone results in less mortality than mitoxantrone in doxorubicin-pretreated mice. Pixantrone (16.25 mg/kg i.v, q7d × 3) modulates Lymph node cells (LNC) responses, and affacts T cell subpopulations in TAChR-immunized Lewis rats. Pixantrone also shows preventive and therapeutic effect in experimental autoimmune myasthenia gravis (EAMG) rats. |
Pixantrone maleate - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.795 ml | 8.973 ml | 17.947 ml |
| 5 mM | 0.359 ml | 1.795 ml | 3.589 ml |
| 10 mM | 0.179 ml | 0.897 ml | 1.795 ml |
| 5 mM | 0.036 ml | 0.179 ml | 0.359 ml |
Last Update：2024-01-02 23:10:35
Pixantrone maleate - Reference Information
| biological activity | Pixantrone (BBR-2778) is a new type of aza-anthracenedione compound with anti-tumor activity. It has weak inhibitory activity on topoisomerase II, and forms DNA adduct by alkylation of DNA hypermethylation sites. |
| target | TargetValue Topo II () |
| Target | Value |
| in vitro study | Pixantrone dimaleate is a topoisomerase II inhibitor. Pixantrone induces cell death in multiple cancer cell lines independent of cell perturbation, with IC 50 s of 37.3 nM, 126 nM and 136 nM for T47D, MCF-10A and OVCAR5 cells, respectively. Pixantrone induces DNA damage at high concentrations (500 nM) but not at concentrations (100 nM) sufficient to kill PANC1 cells. Pixantrone (25 or 100 nM) induces severe chromosomal aberrations and mitotic catastrophe in PANC1 cells. Pixantrone (100 nM) may disrupt chromosome segregation because of generating merotelic kinetochore attachments that cause chromosome non-disjunction. Pixantrone potently inhibits growth of human Leukemia K562 cells, etoposide-resistant K/VP. 5 cells, MDCK and ABCB1-transfected MDCK/MDR cells, with IC 50 s of 0.10 μ m, 0.56 μ m, 0.058 μ m and 4.5 μ m, respectively. Pixantrone (0.01-0.2 μ m) led to a concentration-dependent formation of linear DNA through acting on topoisomerase II α. Pixantrone produces semiquinone free radicals in an enzymatic reducing system, although not in a cellular system, most likely due to low cellular uptake. Pixantrone (0.01-10 μ m) shows potent inhibitory activities against rat 97-116 peptide-specific T cell proliferation. |
| in vivo study | Pixantrone (27 mg/kg) does not worsen pre-existing moderate degenerative cardiomyopathy in doxorubicin-pretreated mice, by I. v. one dose every 7 days repeated thrice (q7d × 3). Pixantrone (27 mg/kg) uses minimal cardiotoxic in mice following repeated treatment cycles. Moreover, Pixantrone results in less mortality than mitoxantrone in doxorubicin-pretreated mice. Pixantrone (16.25 mg/kg I. v, q7d × 3) modulates Lymph node cells (LNC) responses, and affacts T cell subpopulations in TAChR-immunized Lewis rats. Pixantrone also shows preventive and therapeutic effect in experimental autoimmune myasthenia gravis (EAMG) rats. |
Last Update：2024-04-09 02:00:00
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Product Name: Pixantrone dimaleate Visit Supplier Webpage Request for quotationCAS: 144675-97-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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