Description
CP-466722, a nontoxic compound, is a ATM protein kinase inhibitor and shows no inhibition to PI3K, PI3K-like protein kinases or Abl kinase in cells.
Storage
2 years at -20 centigrade
Molecular Formula
C17H15N7O2
Chemical Name
2-(6,7-dimethoxyquinazolin-4-yl)-5-(pyridin-2-yl)-2H-1,2,4-triazol-3-amine
Solubility
DSMO 0.28 mg/mL Water
In vitro
CP-466722, a nontoxic compound, is a ATM protein kinase inhibitor and shows no inhibition to PI3K, PI3K-like protein kinases or Abl kinase in cells.CP466722 inhibits ATM function in response to IR-induced DNA damage. As ATM kinase can activate signal transduction pathways essential for coordinating cell cycle progression with DNA repair, CP-466722 induces characteristic cell cycle checkpoint defects by disrupting ATM function and inhibiting cellular ATM-dependent phosphorylation. Removing CP466722 lead to reversion of inhibition of cellular ATM kinase activity.
In vivo
While KU-55933 did not enhance TMZ induced Chk1/Chk2 activation, it increased TMZ-induced residual gamma-H2AX foci in the parental cells but not in the TMZ resistant cells. Similar sensitization was observed with CP-466722 combined with TMZ in GBM12 xenograft line but not in GBM12TMZ, which is resistant to TMZ due to MGMT overexpression.
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