In vivo studies involving nude mice implanted with human colon tumor (HCT116) xenografts demonstrate that a single intraperitoneal (i.p.) dose of GSK-1070916 dose-dependently inhibits HH3-S10 phosphorylation. Further, repeated i.p. administrations of GSK-1070916 have resulted in either complete or partial antitumor activity in various types of tumors, including lung (A549), colon (HCT116), acute myelogenous leukemia (AML, HL60), and chronic myelogenous leukemia (CML, K562). The compound also stabilized disease in colon (Colo205), lung (H460), and breast (MCF-7) tumors and delayed tumor growth in another colon model (SW620). The daily administration of GSK-1070916 was generally well-tolerated in these animal models^[2].

GSK-1070916 effectively inhibits Aurora B/INCENP and Aurora C/INCENP kinases with dissociation constants (Kis) of 0.38±0.29 nM and 1.45±0.35 nM, respectively, demonstrating lesser potency against Aurora A/TPX2 with a Ki of 492±61 nM. Additionally, this compound shows inhibitory activity against FLT1, TIE2, SIK, FLT4, and FGFR1, with IC50 values of 42, 59, 70, 74, and 78 nM, respectively. In A549 human lung cancer cells, GSK-1070916 exhibits a strong antiproliferative effect, with an EC50 of 7 nM^[1].

GSK-1070916 has been tested across a range of tumor cell lines, showing consistent inhibition of the phosphorylation of histone H3 at serine 10 (HH3-S10), with average EC50 values spanning from 8 to 118 nM^[2].