Barasertib, also known as AZD-1152, is a highly selective aurora kinase B inhibitor. As an aurora kinase inhibitor, it has shown the ability to disrupt the cell cycle and consequently induce apoptosis in vitro. It has inhibited the growth of human colon, lung, and haematologic tumor xenografts in immunodeficient mice, and continues to be evaluated in various disease models.
In a 2016 study, barasertib inhibited the growth of small-cell lung cancer cells in vitro and in vivo. Small-cell lung cancer cells are good targets for aurora kinase inhibition, thanks to their rapid proliferation and high rates of MYC family amplification. Inhibitors of mitosis such as aurora kinase inhibitors have been effective in causing apoptosis in cells expressing high levels of MYC in other tumor types.
A panel of small-cell lung cancer lines with and without MYC family gene amplification was screened for growth inhibition by barasertib. The growth inhibition caused by barasertib correlated with cMYC amplification and cMYC gene expression in the panel. Small-cell lung cancer tumors with high cMYC amplification or gene expression may thus be good targets for barasertib and other aurora kinase B inhibitors.
LKT Labs sells a number of aurora kinase inhibitors, including AZD1152:
References:
Helfrich B., Kim J., et al. Barasertib (AZD1152), a Small Molecule Aurora B Inhibitor, Inhibits the Growth of SCLS Cell Lines In Vitro and In Vivo. Mol Cancer Ther; 15(10); 2314-22. PMID: 27496133.