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KU-60019

Cat. No. M1998
KU-60019 Structure
Size Price Availability Quantity
5mg USD 67.5  USD75 In stock
10mg USD 90  USD100 In stock
50mg USD 270  USD300 In stock
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Quality Control
Biological Activity

KU-60019 is a potent ATM kinase inhibitor with IC50 of 6.3 nM. KU-60019 exhibits little to no nonspecific target effects, displaying similar target selectivity to KU 55933. KU-60019 inhibited the phosphorylation of the major DNA damage effectors p53, H2AX and KAP1 as well as AKT. 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 has also been shown to Inhibit invasion and migration of human glioma cells in vitro. KU-60019 is 10-fold more effective than KU-55933 at blocking radiation-induced phosphorylation of key ATM targets in human glioma cells. 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.

Product Citations
Customer Product Validations & Biological Datas
Source Med Sci Monit (2017). Figure 4.KU-60019
Method Proliferation assay
Cell Lines PA-SMCs
Concentrations 0.1 μM, 0.3 μM, 0.5 μM
Incubation Time 24 h
Results The results demonstrated that at a concentration of 0.5 μM, KU60019 increased cell growth more noticeably compared with other groups
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 547.67
Formula C30H33N3O5S
CAS Number 925701-49-1
Purity 99.15%
Solubility DMSO 40 mg/mL
Storage at -20°C
References

Dynamic inhibition of ATM kinase provides a strategy for glioblastoma multiforme radiosensitization and growth control.
Golding SE, et al. Cell Cycle. 2012 Mar 15;11(6):1167-73. PMID: 22370485.

Improved ATM kinase inhibitor KU-60019 radiosensitizes glioma cells, compromises insulin, AKT and ERK prosurvival signaling, and inhibits migration and invasion.
Golding SE, et al. Mol Cancer Ther. 2009 Oct;8(10):2894-902. PMID: 19808981.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: KU-60019 supplier, ATM/ATR, inhibitors

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