Pixantrone

• CAT Number: I001709
• CAS Number: 144510-96-3
• Molecular Formula: C17H19N5O2
• Molecular Weight: 325.37
• Purity: ≥95%
• Target: Topoisomerase
• Solubility: 10 mM in DMSO
• Storage: -20°C

Pixantrone (BBR 2778) is an experimental antineoplastic drug.Target: OthersPixantrone is an experimental antineoplastic (anti-cancer) drug, an analogue of mitoxantrone with fewer toxic effects on cardiac tissue, It acts as a topoisomerase II poison and intercalating agent. Pixantrone may be useful in patients pretreated with anthracyclines [1]. An in vitro crosslinking assay demonstrated that Pixantrone is efficiently activated by formaldehyde to generate covalent drug-DNA adducts capable of stabilizing double-stranded DNA in denaturing conditions. Pixantrone-DNA adduct formation is both concentration and time dependent and the reaction exhibits an absolute requirement for formaldehyde. Pixantrone exhibited a 10- to 100-fold greater propensity to generate adducts at equimolar formaldehyde and drug concentrations. Pixantrone-DNA adducts are thermally and temporally labile, yet they exhibit a greater thermal midpoint temperature and an extended half-life at 37 degrees C when compared to mitoxantrone-DNA adducts [2].

Reference

[1]. 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. 25(3): p. 187-95.

[2]. Evison, B.J., et al., Pixantrone can be activated by formaldehyde to generate a potent DNA adduct forming agent. Nucleic Acids Res, 2007. 35(11): p. 3581-9.