Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
1 mg
5 mg
10 mg
1 mM
2.1253 mL
10.6265 mL
21.2531 mL
5 mM
0.4251 mL
2.1253 mL
4.2506 mL
10 mM
0.2125 mL
1.0627 mL
2.1253 mL
50 mM
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Description
ETP-46464 is a potent and selective inhibitor of with of 25 nM.
Features
Selective ATR inhibitor and particularly toxic to p53-deficient cancer cells. Often used as a pharmacologic probe due to its ideal pharmacological properties.
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.