KU-60019

Catalog No.S1570

KU-60019 Chemical Structure

Molecular Weight(MW): 547.67

KU-60019 is an improved analogue of KU-55933, with IC50 of 6.3 nM for ATM in cell-free assays, 270- and 1600-fold more selective for ATM than DNA-PK and ATR,and is a highly effective radiosensitizer.

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In DMSO USD 195 In stock
USD 150 In stock
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Cited by 52 Publications

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Choose Selective ATM/ATR Inhibitors

Biological Activity

Description KU-60019 is an improved analogue of KU-55933, with IC50 of 6.3 nM for ATM in cell-free assays, 270- and 1600-fold more selective for ATM than DNA-PK and ATR,and is a highly effective radiosensitizer.
Features Improved analog of KU-55933, and is more effective at blocking ATM-mediated DDR events.
Targets
ATM [1]
(Cell-free assay)
6.3 nM
In vitro

Compared to KU-55933, KU-60019 is an improved more water-soluble inhibitor of the ATM kinase, while displaying similar target selectivity. KU-60019 has little activity against DNA-PKcs and ATR with IC50 values of 1.7 μM and >10 μM, respectively, as well as 229 other protein kinases such as PI3K, mTOR and mTOR/FKBP12. KU-60019 displays 3- to 10-fold more potency than KU-55933 at blocking radiation-induced phosphorylation of key ATM protein targets such as p53, γ-H2AX, and CHK2, in human glioma U87 and U1242 cells, as 1 μM of KU-60019 significantly induces >70% decrease of p53 (S15) phosphorylation to which extent ~10 μM of KU-55933 is required to achieve. KU-60019 effectively radiosensitizes human glioma cells with dose-enhancement ratio of 1.7 and 4.4 at 1 μM and 10 μM, respectively, and also radiosensitizes the normal fibroblasts but not the A-T fibroblasts. KU-60019 treatment (3 μM) blocks basal and insulin-induced AKT S473 phosphorylation by 70% and ~50%, respectively, and completely reduces radiation-induced AKT phosphorylation below the level of control. The effect of KU-60019 on AKT S473 phosphorylation can be seen in glioma cell lines and normal fibroblasts but not in A-T (h-TERT) cells, and can be significantly blocked by phosphatase inhibitor okadaic acid, suggesting a critical role of ATM kinase in regulating AKT phosphorylation via unknown phosphatase. Consistent with the inhibition of prosurvival AKT signaling, KU-60019 at 3 μM significantly inhibits migration and invasion of human glioma U87 cells by >70% and ~60%, respectively, as well as U1242 cells by >50% and ~60% respectively. [1]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BAECs NWT0OnBITnWwY4Tpc44hSXO|YYm= NXLxdGI1OTEEoN88US=> NGTLdpkyyqCqwrC= NXXMe2pRTE2VTx?= MUnhZo9tcXOqZYOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDVF2tV4VzOTl6MR?= M3\O[FI2PDl6NUSy
BAECs MV\GeY5kfGmxbjDBd5NigQ>? Mnz3NVDDqM7:TR?= MYixxsBpyqB? MUTEUXNQ M1\kZYlvcGmkaYTzJJRp\SCrbnPy[YF{\SCrbjDOU3Mh[WO2aY\peJk> MofINlU1QTh3NEK=
U1242 MUXLbY5ie2ViQYPzZZk> MVezJO69VcLi NHrDXGcxNjViaB?= MU\EUXNQ NF2yWYXDqGmwaHnibZR{KHSqZTDBWG0hc2mwYYPl MlLINlM3OjB2MEm=
U87 NVP6OHh4U2mwYYPlJGF{e2G7 NGC4PZc{KM7:TdMg MWOwMlUhcA>? NUja[|ByTE2VTx?= NUizXZdWyqCrbnjpZol1eyC2aHWgRXROKGurbnHz[S=> M3XtTVI{PjJyNEC5
U1242 NEjxOpFCeG:ydH;zbZMhSXO|YYm= NXHZNGlpOyEQvF5CpC=> M2DmdVHDqGkEoB?= MXjEUXNQ M4f1b5Ji\Gmxc3Xud4l1cXqnczDoeY1idiCpbHnvcYEh[2WubIO= Mn\WNlM3OjB2MEm=
U87 MmPFRZBweHSxc3nzJGF{e2G7 NXXmNGhNOyEQvF5CpC=> M1\LWlHDqGkEoB?= NF\tS5ZFVVOR MVLyZYRqd3OnboPpeIl7\XNiaIXtZY4h\2yrb33hJINmdGy| NFzKR|EzOzZ{MESwPS=>
U1242  M3nSNGtqdmG|ZTDBd5NigQ>? NIXrTGQxNjBzLUOg{txOyqB? MlX0NUBp NGXsdnJFVVOR NUKyZ41N[myxY3vzJGFVVSCtaX7hd4Uh[WO2aY\peJkh[XRibH;3JINwdmOnboTyZZRqd26| M4n4dVIzOzdyNEi1

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-ATM / ATM / p-AKT / AKT / PKM2 ; 

PubMed: 30799198     


CAFs (Cancer-associated fibroblasts) were cultured in normoxia or hypoxia for 8 h and treated with or without KU60019 (5 μM), protein levels of p-ATM, ATM, p-AKT, AKT and PKM2 were determined by Western blotting.

30799198
Immunofluorescence
GLUT1; 

PubMed: 30799198     


CAFs (Cancer-associated fibroblasts) were cultured in normoxia or hypoxia for 8 h and treated with or without KU60019 (5 μM), the membrane GLUT1 was shown by immunofluorescence staining. Scale bar, 50 μm. 

30799198
In vivo In orthotopic glioma U1242/luc-GFP xenograft models, the combination of KU-60019 and radiation significantly increases survival of mice than KU-60019 alone, radiation alone, or no treatment. In addition, p53-mutant gliomas is much more sensitive to KU-60019 radiosensitization than wild-type glioma. [2]

Protocol

Cell Research:[1]
- Collapse
  • Cell lines: U87 and U1242
  • Concentrations: Dissolved in water, final concentrations ~3 μM
  • Incubation Time: 1, 3, and 5 days
  • Method: Cells are exposed to KU-60019 for 1, 3, and 5 days. Cell growth is determined by AlamarBlue. AlamarBlue is added to the medium to the recommended final concentration. Plates are incubated for 1 hour at 37 °C, fluorescence is determined on a Fluoro-Count plate reader (excitation 530 nm, emission 590 nm), and values are taken as a measure of cell growth. Cell survival is determined by trypan blue/fluorescence activated cell sorting (FACS) assay.
    (Only for Reference)
Animal Research:[2]
- Collapse
  • Animal Models: Athymic female mice harboring orthotopic glioma U1242/luc-GFP tumors or human glioma U1242/luc-GFP tumors
  • Formulation: PBS
  • Dosages: KU-60019 (10 μM) is delivered at a rate of 0.5 μL/h by osmotic pump; KU-60019 (250 μM) in 12.5 μL is infused by CED.
  • Administration: Administered intratumorally by convection-enhanced delivery or osmotic pump
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 18 mg/mL warmed (32.86 mM)
Water Insoluble
Ethanol Insoluble

* 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 547.67
Formula

C30H33N3O5S
CAS No. 925701-49-1
Storage powder
in solvent
Synonyms N/A

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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:

    what vehicle do you recommend for in vivo use of this compound?

  • Answer:

    The formula for i.p. injections: 5% stock solution (100mg/ml) +30% PEG 300+ddH2O could reach a final concentration of 5mg/ml.

selleck catalog

ATM/ATR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID