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

500508
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₃₀H₂₂N₄O₂ 1345675-02-7

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      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.00508.0001
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          Glass bottle 10 mg
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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
          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

          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.