KU-0060648

Catalog No.S8045

KU-0060648 Chemical Structure

Molecular Weight(MW): 582.71

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.

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Biological Activity

Description 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.
Targets
PI3Kδ [1] PI3Kβ [1] PI3Kα [1] DNA-PK [2] PI3Kγ [1]
0.1 nM 0.5 nM 4 nM 8.6 nM 0.59 μM
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]

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: MCF7, T47D, MDA-MB-231, LoVo and SW620
  • Concentrations: ~1 μM
  • Incubation Time: 5 day
  • Method: SRB assay
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: human-tumor SW620 or MCF7 xenograft models
  • Formulation: Saline
  • Dosages: 10 mg/kg, twice daily
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 0.4 mg/mL (0.68 mM)
Water slightly soluble or insoluble
Ethanol slightly soluble or insoluble
In vivo Add solvents individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W
20 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 582.71
Formula

C33H34N4O4S

CAS No. 881375-00-4
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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DNA-PK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID