An ATR inhibitor
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ETP-46464

Item No. 19809

Technical Information
Formal Name
α,α-dimethyl-4-[2-oxo-9-(3-quinolinyl)-2H-[1,3]oxazino[5,4-c]quinolin-1(4H)-yl]-benzeneacetonitrile
CAS Number
1345675-02-6
Synonyms
  • ATM Inhibitor III
  • ATR Inhibitor III
Molecular Formula
C30H22N4O2
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 20 mg/mLDMF:PBS (pH 7.2) (1:4): 0.2 mg/mLDMSO: 12 mg/mL
λmax
261, 323 nm
SMILES
O=C1OCC(C=NC2=C3C=C(C4=CC(C=CC=C5)=C5N=C4)C=C2)=C3N1C6=CC=C(C(C)(C)C#N)C=C6
InChi Code
InChI=1S/C30H22N4O2/c1-30(2,18-31)23-8-10-24(11-9-23)34-28-22(17-36-29(34)35)16-33-27-12-7-19(14-25(27)28)21-13-20-5-3-4-6-26(20)32-15-21/h3-16H,17H2,1-2H3
InChi Key
DPLMXAYKJZOTKO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    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.

    References & Product Citations
    Product Description References

    1. Toledo, L.I., Murga, M., Zur, R., et alA cell-based screen identifies ATR inhibitors with synthetic lethal properties for cancer-associated mutations. Nat. Struct. Mol. Biol. 18(6), 721-727 (2011).