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KU-60019ATM kinase inhibitor,potent and selective

KU-60019

Catalog No. A8336
Size Price Stock Qty
10mM (in 1mL DMSO) $85.00 In stock
10mg $98.00 In stock
50mg $300.00 In stock
200mg $900.00 In stock

Tel: +1-832-696-8203

Email: sales@apexbt.com

Worldwide Distributors

Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Caster JM, Yu SK, et al. "Effect of particle size on the biodistribution, toxicity, and efficacy of drug-loaded polymeric nanoparticles in chemoradiotherapy." Nanomedicine. 2017 Mar 11. pii: S1549-9634(17)30044-8. PMID:28300658

Quality Control

Chemical structure

KU-60019

Related Biological Data

KU-60019

Related Biological Data

KU-60019

Related Biological Data

KU-60019

Biological Activity

Description KU-60019 is an improved analogue of KU-55933 with IC50 of 6.3 nM for ATM, 270- and 1600-fold more selective for ATM than DNA-PK and ATR.
Targets ATM          
IC50 6.3 nM          

Protocol

Cell experiment [1]:

Cell lines

U87 and U1242 cells

Preparation method

The solubility of this compound in DMSO is > 27.4 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

3 μM; 1, 3 and 5 days

Applications

In U87 cells, KU-60019 at 3 μM significantly inhibited cell migration and invasion by > 70% and ~ 60%, respectively. Similarly, KU-60019 also substantially inhibited migration and invasion of human glioma U1242 cells by > 50% and ~ 60%, respectively.

Animal experiment [2]:

Animal models

Athymic female mice implanted with U1242/luc-GFP cells

Dosage form

KU-60019 (10 μM) delivered intratumorally at a rate of 0.5 μL/h by osmotic pump, for 14 days

Applications

In athymic female mice implanted with U1242/luc-GFP cells, the combination of KU-60019 and radiation significantly inhibited tumor growth than radiation alone, which suggested that KU-60019 might radiosensitize U1242 gliomas.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Golding SE1, Rosenberg E, Valerie N, Hussaini I, Frigerio M, Cockcroft XF, Chong WY, Hummersone M, Rigoreau L, Menear KA, O'Connor MJ,Povirk LF, van Meter T, Valerie K. Improved ATM kinase inhibitor KU-60019 radiosensitizes glioma cells, compromises insulin, AKT and ERK prosurvival signaling, and inhibits migration and invasion. Mol Cancer Ther. 2009 Oct;8(10):2894-902.

[2]. Biddlestone-Thorpe L, Sajjad M, Rosenberg E, Beckta JM, Valerie NC, Tokarz M, Adams BR, Wagner AF, Khalil A, Gilfor D, Golding SE, Deb S, Temesi DG, Lau A, O'Connor MJ, Choe KS, Parada LF, Lim SK, Mukhopadhyay ND, Valerie K. ATM kinase inhibition preferentially sensitizes p53-mutant glioma to ionizing radiation. Clin Cancer Res. 2013 Jun 15;19(12):3189-200.

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Chemical Properties

Cas No. 925701-49-1 SDF Download SDF
Synonyms KU60019;KU 60019
Chemical Name 2-[(2S,6R)-2,6-dimethylmorpholin-4-yl]-N-[5-(6-morpholin-4-yl-4-oxopyran-2-yl)-9H-thioxanthen-2-yl]acetamide
Canonical SMILES CC1CN(CC(O1)C)CC(=O)NC2=CC3=C(C=C2)SC4=C(C=CC=C4C3)C5=CC(=O)C=C(O5)N6CCOCC6
Formula C30H33N3O5S M.Wt 547.68
Solubility >27.4mg/mL in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

KU-60019 is a selective inhibitor of the Ataxia telangiectasia (A-T) mutated (ATM) protein with an IC50 value of 6.3 nM. In literature report, KU-60019 radiosensitizes h-TERT-immortalized normal fibroblasts but not A-T fibroblasts, suggesting it is a specific ATM kinase radiosensitizer [1].

KU-60019 can reduce radiation-induced S473 AKT phosphorylation in human glioma cell lines that are p53 wild type (U87) and p53 mutant (U1242). However, the suppression of AKT does not enhance radiosensitization of KU-60019 [1].

KU-60019 has been reported to inhibit cell migration and invasion in human glioma cells U87 and U1242 in a dose-dependent manner. Besides, KU-60019, to some extent, has also been shown to suppress the growth of U1242 cells [1].

References:
[1] Golding SE1, Rosenberg E, Valerie N, Hussaini I, Frigerio M, Cockcroft XF, Chong WY, Hummersone M, Rigoreau L, Menear KA, O'Connor MJ,Povirk LF, van Meter T, Valerie K. Improved ATM kinase inhibitor KU-60019 radiosensitizes glioma cells, compromises insulin, AKT and ERK prosurvival signaling, and inhibits migration and invasion. Mol Cancer Ther. 2009 Oct;8(10):2894-902.