| Name | KU-0060648 |
| Description | KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 values of 8.6 nM, 4 nM, 0.5 nM, and 0.1 nM respectively, and demonstrates less inhibition of PI3Kγ with an IC50 of 0.59 μM. |
| Cell Research | SRB assay(Only for Reference) |
| In vitro | 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] |
| In vivo | 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] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | 2eq.HCl : 58.3 mg/mL (100 mM)
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| Keywords | mTOR | KU-0060648 | inhibit | Phosphoinositide 3-kinase | Inhibitor | Mammalian target of Rapamycin | DNA-PK | KU 0060648 | DNA-dependent protein kinase | PI3K |
| Inhibitors Related | L-Leucine | Capivasertib | Myricetin | Erucic acid | Sapanisertib | (2S,3R,4S)-4-Hydroxyisoleucine | Duvelisib (R enantiomer) hydrochloride | Isoprenaline hydrochloride | Quercetin | Quercetin Dihydrate | Rapamycin | Apilimod |
| Related Compound Libraries | Glycolysis Compound Library | Bioactive Compound Library | Antidepressant Compound Library | Kinase Inhibitor Library | Antioxidant Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Neuronal Differentiation Compound Library |
United States
