CAS144675-97-8
EINECS680-661-5化學(xué)式C21H23N5O6
分子量441.43722InChIInChI=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+熔點(diǎn)192°沸點(diǎn)650°C at 760 mmHg閃點(diǎn)346.9°C蒸汽壓8.89E-17mmHg at 25°C溶解度DMSO: 33.33毫克/毫升 (59.78毫米; 需要超聲波) H2O: 16.67毫克/毫升 (29.90毫米;需要超聲波)存儲(chǔ)條件under inert gas (nitrogen or Argon) at 2-8°C體外研究Pixantrone dimaleate is a topoisomerase II inhibitor. Pixantroneinduces cell death in multiple cancer cell lines independent ofcell cycle perturbation, with IC 50 s of 37.3 nM, 126 nM and 136 nMfor T47D, MCF-10A and OVCAR5 cells, respectively. Pixantroneinduces DNA damage at high concentrations (500 nM) but not atconcentrations (100 nM) sufficient to kill PANC1 cells. Pixantrone(25 or 100 nM) induces severe chromosomal aberrations and mitoticcatastrophe in PANC1 cells. Pixantrone (100 nM) may disruptchromosome segregation because of generating merotelic kinetochoreattachments that cause chromosome non-disjunction. Pixantronepotently inhibits growth of human Leukemia K562 cells,etoposide-resistant K/VP.5 cells, MDCK and ABCB1-transfectedMDCK/MDR cells, with IC 50 s of 0.10 μM, 0.56 μM, 0.058 μM and 4.5μM, respectively. Pixantrone (0.01-0.2 μM) leads to aconcentration-dependent formation of linear DNA through acting ontopoisomerase IIα. Pixantrone produces semi free radicals inan 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 97-116peptide-specific T cell proliferation.