中文名 | 马来到匹杉琼 |
英文名 | Benz(g)isoquinoline-5,10-dione, 6,9-bis((2-aminoethyl)amino)-, (2Z)-2- butenedioate (1:2) |
别名 | 马来到匹杉琼 马来酸匹衫群 匹杉群马来酸盐 匹杉琼马来酸盐 马来酸匹克生琼 马来酸盐匹杉琼 匹杉群二马来酸盐 匹克生琼马来酸盐 马来到匹杉琼(PX) |
英文别名 | 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 |
化学式 | C21H23N5O6 |
分子量 | 441.43722 |
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+ |
熔点 | 192° |
沸点 | 650°C at 760 mmHg |
闪点 | 346.9°C |
蒸汽压 | 8.89E-17mmHg at 25°C |
溶解度 | DMSO: 33.33毫克/毫升 (59.78毫米; 需要超声波) H2O: 16.67毫克/毫升 (29.90毫米; 需要超声波) |
存储条件 | under inert gas (nitrogen or Argon) at 2-8°C |
体外研究 | 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. |
体内研究 | 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. |
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 |
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