Abstract 3770: PK/PD/Efficacy characterization of AZ285, a selective CK2 kinase inhibitor

Proceedings: AACR 103rd Annual Meeting 2012‐‐ Mar 31‐Apr 4, 2012; Chicago, IL Casein Kinase 2 (CK2) is an abundant, highly conserved protein serine/threonine kinase with numerous physiological targets and participates in the maintenance of cell viability with a role in cell growth and proliferation. While the expression level of CK2 in normal cells is tightly regulated, there is an increasing body of evidence demonstrating it's over expression in cancerous cells, thereby making inhibition a viable chemotherapeutic target. Here we will describe a mathematical tumor growth inhibition model describing the relationship between systemic exposure to a potent inhibitor of CK2 (AZ285) and efficacy in the HCT116 xenograft model. Furthermore, a PK/PD model describing the onset, intensity, and duration of the pAKT and cleaved caspase 3 response as function of concentration and time is described and linked to pre-clinical xenograft efficacy outcomes. Citation Format: {Authors}. {Abstract title} [abstract]. In: Proceedings of the 103rd Annual Meeting of the American Association for Cancer Research; 2012 Mar 31-Apr 4; Chicago, IL. Philadelphia (PA): AACR; Cancer Res 2012;72(8 Suppl):Abstract nr 3770. doi:1538-7445.AM2012-3770