Home PI3K/Akt/mTOR DNA-PK inhibitor - PI3K inhibitor KU-0060648 For research use only.

KU-0060648

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 Chemical Structure

KU-0060648 Chemical Structure

CAS No. 881375-00-4

Purity & Quality Control

KU-0060648 Related Products

Signaling Pathway

DNA-PK Signaling Pathways

DNA-PK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HeLa cells Function assay Inhibition of DNA-PK autophosphorylation at S2056 in human HeLa cells, EC50=0.136 μM 23855836
MO59J-Fus1 cells Function assay 1 μM Inhibition of human DNA-PK autophosphorylation at S2056 in MO59J-Fus1 cells at 1 uM 23855836
HeLa Function assay Inhibition of DNA-PK autophosphorylation at S2056 in human HeLa cells, EC50 = 0.136 μM. 23855836
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
HeLa Function assay 1 uM 1 hr Inhibition of DNA-PK in human HeLa cells assessed as phosphorylation of gammaH2AX at 1 uM treated 1 hr before 5 Gy ionizing radiation measured within 30 mins by immunofluorescence assay 23855836
Click to View More Cell Line Experimental Data

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]
(Cell-free assay)		 PI3Kβ [1]
(Cell-free assay)		 PI3Kα [1]
(Cell-free assay)		 DNA-PK [1]
(Cell-free assay)		 PI3Kγ [1]
(Cell-free assay)
0.1 nM 0.5 nM 4 nM 5 nM 0.59 μM
In vitro
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. 
Cell Research Cell lines MCF7, T47D, MDA-MB-231, LoVo and SW620
Concentrations ~1 μM
Incubation Time 5 day
Method

SRB assay

Chemical Information & Solubility

Molecular Weight 582.71 Formula

C33H34N4O4S
CAS No. 881375-00-4 SDF Download KU-0060648 SDF
Smiles CCN1CCN(CC1)CC(=O)NC2=C3C4=CC=CC=C4SC3=C(C=C2)C5=CC=CC6=C5OC(=CC6=O)N7CCOCC7
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 2 mg/mL ( (3.43 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

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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Frequently Asked Questions

Question 1:
On your product page the in vivo solubility for S8045 in 30% Propylene glycol, 5% Tween 80, 65% D5W is up to 20 mg/mL, but in the reference listed "Chemosensitization of cancer cells by KU-0060648, a dual inhibitor of DNA-PK and PI-3K." they use Phosphoric Acid pH 5 to resuspend the drug. I am curious if you have any information on solubility in phosphoric acid pH 5 for KU0060648.

Answer:
30% Propylene glycol, 5% Tween 80, 65% D5W to 20 mg/mL is the vehicle we tested in our lab, it's a suspension and can only be used as oral gavage. Phosphoric Acid pH 5 is from the reference, but we didn't test the solubility of our compound in it.

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