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ETP-46464 1345675-02-6

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Synonyms
Appearance
Chemical Formula
C30H22N4O2
Solubility
Molecular Weight
470.52
Storage and Stability
in stock
CAS No.
1345675-02-6
Purity
98%+
Introduction
ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.

ETP-46464 shows almost full activity against ATR at 100 nM. ETP-46464 inhibits the activity of PI3Kα, mTOR and DNA-PKcs with IC50s of 170, 0.6 and 36 nM. ETP-46464 is able to promote the breakage of stalled replication forks. Exposure to ETP-46464 leads the generation of substantial amounts of DNA damage in replicating cells. 1 μM ETP-46464 abrogates the ionizing radiation-induced G2/M checkpoint and leads to the presence of micronuclei or completely fragmented nuclei in cells. ETP-46464 is particularly toxic for p53-deficient cells, which is exacerbated by replicative stress-generating conditions such as the overexpression of cyclin E. [1]

 
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