Pixantrone-d8 (maleate)

Pixantrone-d₈ is intended for use as an internal standard for the quantification of pixantrone by GC- or LC-MS. Pixantrone is a DNA topoisomerase II inhibitor.¹ It induces SV40 DNA cleavage in the presence of mouse topoisomerase II and induces DNA single-strand breaks in NCI H187 cells in a concentration-dependent manner. Pixantrone is cytotoxic to L1210 leukemia cells as well as doxorubicin-sensitive and -resistant LoVo colon adenocarcinoma cells (IC₅₀ = 0.01, 0.24, and 7.2 µg/ml, respectively).² It decreases disease severity in a rat model of myasthenia gravis induced by immunization with the T. californica acetylcholine receptor (AChR) when administered at a dose of 8.12 mg/kg once per week for six weeks.³ Formulations containing pixantrone have been used in the treatment of non-Hodgkin B cell lymphoma.

1.De Isabella, P., Palumbo, M., Sissi, C., et al.Topoisomerase II DNA cleavage stimulation, DNA binding activity, cytotoxicity, and physico-chemical properties of 2-aza- and 2-aza-oxide-anthracenedione derivativesMol. Pharmacol.48(1)30-38(1995) 2.Krapcho, A.P., Petry, M.E., Getahun, Z., et al.6,9-Bis[(aminoalkyl)amino]benzo[g]isoquinoline-5,10-diones. A novel class of chromophore-modified antitumor anthracene-9,10-diones: Synthesis and antitumor evaluationsJ. Med. Chem.37(6)828-837(1994) 3.Marolda, R., Ruocco, C., Cordiglieri, C., et al.Differential targeting of immune-cells by Pixantrone in experimental myasthenia gravisJ. Neuroimmunol.258(1-2)(2013)