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    PI3K/Akt/mTOR
  2. ATM/ATR
  3. KU-60019

KU-60019 

Cat. No.: HY-12061 Purity: 98.96%
Handling Instructions

KU-60019 is an improved ATM kinase-specific inhibitor with IC50 of 6.3 nM.

For research use only. We do not sell to patients.

KU-60019 Chemical Structure

KU-60019 Chemical Structure

CAS No. : 925701-46-8

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10 mM * 1 mL in DMSO USD 101 In-stock
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5 mg USD 84 In-stock
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10 mg USD 119 In-stock
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50 mg USD 360 In-stock
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100 mg USD 600 In-stock
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Based on 5 publication(s) in Google Scholar

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Description

KU-60019 is an improved ATM kinase-specific inhibitor with IC50 of 6.3 nM.

IC50 & Target[1]

ATM

6.3 nM (IC50)

DNA-PKcs

1.7 μM (IC50)

In Vitro

KU-60019 is an improved analogue of KU-55933. KU-55933 has an IC50 of 13 nM and Ki of 2.2 nM in vitro and is highly specific for the ATM kinase using a panel of 60 protein kinases. KU-60019 is an improved inhibitor of the ATM kinase with an IC50 of 6.3 nM, approximately half that of KU-55933. The IC50 values for DNA-PKcs and ATR are 1.7 and >10 μM, respectively, almost 270-and 1600-fold higher than for ATM. KU-60019 is 10-fold more effective than KU-55933 at blocking radiation-induced phosphorylation of key ATM targets in human glioma cells. In human U87 glioma cells, KU-55933 completely inhibits phosphorylation of p53 (S15) at 10 μM but not at 3 μM, whereas γ-H2AX levels are only partly reduced with 10 μM 1 h after irradiation. By comparison, 3 μM KU-60019 completely inhibits p53 phosphorylation and partial inhibits at 1 μM[1].

In Vivo

Despite PTEN-deficient control tumors reaching a 4-fold increase in size before PTEN wild-type controls, KU-60019-treated PTEN-deficient tumors display a statistically significant slowing in growth. This growth inhibition is especially evident at the start of the experiment (days 5-12) just after KU-60019 is administered (days 1-5)[2].

Molecular Weight

547.67

Formula

C₃₀H₃₃N₃O₅S

CAS No.

925701-46-8

SMILES

C[[email protected]@H]1O[[email protected]@H](CN(CC(NC2=CC3=C(C=C2)SC4=C(C3)C=CC=C4C5=CC(C=C(O5)N6CCOCC6)=O)=O)C1)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (54.78 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8259 mL 9.1296 mL 18.2592 mL
5 mM 0.3652 mL 1.8259 mL 3.6518 mL
10 mM 0.1826 mL 0.9130 mL 1.8259 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

Cell growth is determined by AlamarBlue. U1242 cells are serially diluted, allowed to attach for 6 h and then exposed to KU-60019 at 3 μM. At days 1, 3 and 5 after seeding, AlamarBlue is added to the medium to the recommended final concentration. Plates are incubated for 1 h at 37°C and fluorescence determined on a FluoroCount plate reader (excitation 530 nm, emission 590 nm) and values taken as a measure of cell growth[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice[2]
Cells (3×107) are implanted into male Fox Chase Severe Combined Immunodeficiency (SCID) mice. Administration of Doxycycline is started when tumors reach 100 mm3 in volume and is performed every 48 hours up to removal of the animal from the experiment. Forty-eight hours after PTEN induction, animals are administered KU-60019 (100 mg/kg) for 5 consecutive days and measured until they reach a target 400 mm3 volume. Measurements of tumor volume and body weight took place every 3 days using calipers.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 98.96%

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KU-60019
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HY-12061
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