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ETP-46464 is an inhibitor of the DNA damage response kinase Ataxia-telangiectasia mutated (ATM)- and Rad3-related (ATR) with an IC50 value of 25 nM.1 It also inhibits mTOR and DNA-dependent protein kinase (IC50s = 0.6 and 36 nM, respectively), and is moderately active against PI3Kα and ATM (IC50s = 170 and 545 nM, respectively).1 Pharmacological inhibition of ATR is reported to generate replicative stress, leading to chromosomal breakage in the presence of conditions that stall replication forks.1 ETP-46464 has been shown to be toxic to p53-deficient cells, which is exacerbated by replicative stress-generating conditions such as the overexpression of cyclin E.1
WARNING This product is not for human or veterinary use.
1. A cell-