KU0060648 是一种PI3K和DNA-PK的双重抑制剂，对 PI3Kα、PI3Kβ、PI3Kδ、PI3Kγ 和 DNA-PK 的IC50值分别为 4 nM、0.5 nM、0.1 nM、0.59 nM 和 8.6 nM。

KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, less inhibition of PI3Kγ with IC50 of 0.59 μM.

KU-0060648 exhibits differential effects on growth inhibition, but is not profoundly cytotoxic in a panel of human cancer cell lines. It inhibits DNA-PK and PI-3K with greater potency in MCF7 than SW620 cell using cell-based assays. Five-day exposure to 1 mM KU-0060648 inhibits cell proliferation by more than 95% in MCF7 cells but only by 55% in SW620 cells. In clonogenic survival assays, KU-0060648 increases the cytotoxicity of etoposide and doxorubicin across the panel of DNA-PKcs-proficient cells, but not in DNA-PKcs-deficient cells, confirming that enhanced cytotoxicity of the topoisomerase II poisons etoposide and doxorubicin is due to DNA-PK inhibition. [1]

KU-0060648 enhances the anti-tumour activity of etoposide in both MCF7 and SW620 xenograft models, and has single-agent activity in the MCF7 xenograft model. [1]

SRB assay(Only for Reference)

881375-00-4

C33H34N4O4S

582.72

KU0060648

2eq.HCl:58.3 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years