ETP-46464是一种有效的，选择性ATR抑制剂，IC50为25 nM。ETP-46464在100nM几乎完全抑制ATR活性。ETP-46464抑制PI3Kα，mTOR和DNA-PKcs蛋白的活性，IC50值分别为170，0.6和36 nM。ETP-46464能够促进复制叉停滞的破损。

98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

ETP46464

DMSO ：6 mg/mL (12.75 mM)

mTOR,ATR,DNA-PK,PI3Kα,ATM

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.

CGK733 does not inhibit ATM or ATR kinase activity in H460 human lung cancer cells.
Choi S,et al. DNA Repair (Amst). 2011 Oct 10;10(10):1000-2. PMID: 21865098