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KI2117ETP-4646410 mg$480

Chemical Characteristic

Product NameETP-46464
SynonymsN/A
CAS No.1345675-02-6
Molecular Weight 470.52
FormulaC30H22N4O2
Chemical Namealpha,alpha-dimethyl-4-(2-oxo-9-(3-quinolinyl)-2h-(1,3)oxazino(5,4-c)quinolin-1(4h)-yl)-benzeneacetonitrile
Smilesc1(ccc(cc1)N1c2c(cnc3c2cc(cc3)c2cnc3c(c2)cccc3)COC1=O)C(C#N)(C)C
Chemical Structure

Biological activities

ETP-46464 is a potent inhibitor of mTOR, ATR, DNA-PK, PI 3-KΑ and ATM. The IC50s of ETP-46464 against mTOR, ATR, DNA-PK, PI 3-Kα and ATM are 0.6, 14, 36, 170 and 545 nM, respectively. In vitro, ETP-46464, at the concentration of 500 nM, preferentially suppresses radiation-induced cellular ATR activity (>90% ) over ATM or DNA-PK activity (IC50 > 5 μM) in U2OS cells, while exhibiting much reduced or little potency toward a panel of 26 other kinases (>55% inhibition at 5 μM).[1]

References

[1] Toledo LI, et al. A cell-based screen identifies ATR inhibitors with synthetic lethal properties for cancer-associated mutations. Nat Struct Mol Biol. 2011, 18(6): 721-727.

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