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KU-60019

Cat. No. M1998

KU-60019 Structure
Size Price Availability Quantity
10mg USD 100 In stock
50mg USD 300 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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.

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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 547.67
Formula C30H33N3O5S
CAS Number 925701-49-1
Purity >99%
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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