500508 ATR Inhibitor III, ETP-46464 - CAS 1345675-02-7 - Calbiochem

500508
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Empirical FormulaCAS #
C₃₀H₂₂N₄O₂ 1345675-02-7

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      Description
      OverviewA cell-permeable quinoline-containing heterotricyclic compound that acts as a potent inhibitor against mTOR, ATR, DNA-PK, PI 3-Kα, and ATM (IC50 = 0.6, 14, 36, 170, and 545 nM, respectively) and preferentially suppresses radiation-induced cellular ATR activity (>90% at 500 nM) 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). Shown to synergize with UCN-01 (Cat. No. 539644) in replicative stress induction in S-phase replicating U2OS (1.5-, 61-, and 190-fold of control RS, respectively, with 1 µM ETP-46464, 50 nM UCN-01, or combined treatment).

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number500508
      Brand Family Calbiochem®
      Synonyms2-methyl-2-(4-(2-oxo-9-(quinolin-3-yl)-2H-[1,3]oxazino[5,4-c]quinolin-1(4H)-yl)phenyl)propanenitrile, ATM and Rad3-Related Inhibitor III, Ataxia-Telangiectasia Mutated Inhibitor III, DNA-PK Inhibitor VI, ATM Inhibitor III, mTOR Inhibitor XIII, PI 3-K Inhibitor XIX, ETP46464
      References
      ReferencesThanasoula, M., et al. 2012. EMBO J. 31, 3398.
      Toledo, L.I., et al. 2011. Nat Struct Mol Biol. 18, 721.
      Product Information
      CAS number1345675-02-7
      FormWhite powder
      Hill FormulaC₃₀H₂₂N₄O₂
      Chemical formulaC₃₀H₂₂N₄O₂
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetATR
      Primary Target IC<sub>50</sub>14 nM
      Purity≥99% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      ATR Inhibitor III, ETP-46464 - CAS 1345675-02-7 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Thanasoula, M., et al. 2012. EMBO J. 31, 3398.
      Toledo, L.I., et al. 2011. Nat Struct Mol Biol. 18, 721.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision09-December-2013 JSW
      Synonyms2-methyl-2-(4-(2-oxo-9-(quinolin-3-yl)-2H-[1,3]oxazino[5,4-c]quinolin-1(4H)-yl)phenyl)propanenitrile, ATM and Rad3-Related Inhibitor III, Ataxia-Telangiectasia Mutated Inhibitor III, DNA-PK Inhibitor VI, ATM Inhibitor III, mTOR Inhibitor XIII, PI 3-K Inhibitor XIX, ETP46464
      DescriptionA cell-permeable quinoline-containing heterotricyclic compound that acts as a potent inhibitor against mTOR, ATR, DNA-PK, PI 3-Kα, and ATM activity (IC50 = 0.6, 14, 36, 170, and 545 nM, respectively, in cell-free kinase assays) and preferentially suppresses ionization radiation/IR-induced cellular ATR activity (>90% inhibition of IR-induced Chk1 pSer345 at 500 nM) over ATM or DNA-PK activity (IC50 > 5 µM against IR-induced ATM pSer189, Chk2 pThr68, DNA-PKcs pSer2056, and γH2AX) in U2OS cells, while exhibiting much reduced or little potency toward a panel of 26 other kinases (>55% inhibition at 5 µM). Shown to synergize with UCN-01 (Cat. No. 539644) in replicative stress/RS induction in S-phase replicating U2OS (% population with pan-nuclear γH2AX staining = 6.0% and 0.2%, respectively, with or without 8 h 5 µM ETP-46464 treatment; 1.5-, 61-, and 190-fold of control RS, respectively, with 1 µM ETP-46464 alone, 50 nM UCN-01 alone, or combined treatment). Likewise, ETP-46464 is also demonstrated to further enhance oncogenic mutations-caused RS elevation in MEF cultures (% RS population without/with 5 µM ETP-46464 treatment = 0.3/0.6, 1.3/2.5, 0.9/3.0, 3.9/11.4, respectively, in wt, p53-/-, Cyclin E-transfected wt, and Cyclin E-transfected p53-/- MEF).
      FormWhite powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1345675-02-7
      Chemical formulaC₃₀H₂₂N₄O₂
      Structure formulaStructure formula
      Purity≥99% by HPLC
      SolubilityDMSO (10 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesThanasoula, M., et al. 2012. EMBO J. 31, 3398.
      Toledo, L.I., et al. 2011. Nat Struct Mol Biol. 18, 721.