On the basis of the in vitro data, it was pivotal to determine if KU0060648 could synergistically promote the antitumor effect of TMZ in vivo. U87 cells were injected subcutaneously into the flank of nude mice, and once tumors grew to approximately 50-75 mm3, mice were randomly treated with KU0060648 (low dose group, 10 mg/kg; high dose group, 50 mg/kg), TMZ (10 mg/kg), or their combination. As shown in Figure 7A, KU0060648 dose-dependently inhibited the growth of U87 tumor. However, 10 mg/kg TMZ alone did not make tumor size regress. Especially, the co-administration of low (10 mg/kg) or high dose (50 mg/kg) of KU0060648 with TMZ resulted in a substantial tumor growth inhibition compared with each agent alone, respectively, confirming that the synergistic effect between KU0060648 and TMZ in vivo. We further address the long-term survival prolonging effect of synergistic KU0060648/TMZ treatment. As shown in Figure 7B, the survival rate of U87 tumor-beard nude mice treated with co-administrated KU0060648/TMZ was profoundly increased compared with each agent alone.