ETP-46464

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. It also inhibits mTOR and DNA-dependent protein kinase (IC50s = 0.6 and 36 nM, respectively), and is moderately active against PI3Kalpha and ATM (IC50s = 170 and 545 nM, respectively). Pharmacological inhibition of ATR is reported to generate replicative stress, leading to chromosomal breakage in the presence of conditions that stall replication forks. 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.Formal Name: alpha,alpha-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: 470.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/mL, DMF:PBS (pH 7.2) (1:4): 0.2 mg/mL, DMSO: 12 mg/mL. lambdamax: 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.