504972 ATR Inhibitor IV - CAS 1232410-49-9 - Calbiochem

504972
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Overview

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Key Specifications Table

Empirical FormulaCAS #
C₁₈H₁₆N₄O₃S 1232410-49-9

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      Description
      OverviewA cell-permeable phenylpyrazine derivative that acts as a potent, ATP-competitive (Ki= 13 nM; IC50/[ATP] = 70 nM/50 µM and 128 nM/100 µM), ATR-selective inhibitor with much reduced or little potency against 4 related PIKKs (Ki= 2.2, 3.9, 16, and >1 µM, respectively, against DNA-PK, PI 3-Kγ, ATM, and mTOR) and 50 other kinases. Shown to selectively inhibit ATR-dependent H2AX Ser139 & Chk1 Ser345 phosphorylation (complete inhibition at 10 µM in HT29 and HFL1 cultures) without affecting ATM- and DNA-PK-mediated H2AX or ATM-mediated Chk2 phosphorylation. Short-term (24 h) VE-821 treatment, either alone or in synergy with Cisplatin (Cat. No. 232120), results in reversible cytostatic growth arrest regardless of cellular ATM-p53 pathway activity, while cytotoxicity and Cisplatin synergism in cell death induction is reported to occur only upon long-term VE-821 exposure (≥72 h) in cultures with ATM-p53 pathway defects.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number504972
      Brand Family Calbiochem®
      SynonymsVE821, 3-amino-6-(4-(methylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide, VE-821, ATM and Rad3-Related Inhibitor IV
      References
      ReferencesPrevo, R., et al. 2012, Cancer Biol. Ther. 13, 1072; Pires, I.M., et al. 2012, Br. J. Cancer 107, 291; Reaper, P.M., et al. 2011, Nat. Chem. Biol. 7, 428.
      Product Information
      CAS number1232410-49-9
      FormYellow solid
      Hill FormulaC₁₈H₁₆N₄O₃S
      Chemical formulaC₁₈H₁₆N₄O₃S
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetATR
      Primary Target K<sub>i</sub>13nM
      Purity≥98% 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 IV - CAS 1232410-49-9 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Prevo, R., et al. 2012, Cancer Biol. Ther. 13, 1072; Pires, I.M., et al. 2012, Br. J. Cancer 107, 291; Reaper, P.M., et al. 2011, Nat. Chem. Biol. 7, 428.
      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.

      Revision03-September-2020 JSW
      SynonymsVE821, 3-amino-6-(4-(methylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide, VE-821, ATM and Rad3-Related Inhibitor IV
      DescriptionA cell-permeable phenylpyrazine derivative that acts as a potent, ATP-competitive (Ki= 13 nM; IC50/[ATP] = 70 nM/50 µM and 128 nM/100 µM), ATR-selective inhibitor with much reduced or little potency against 4 related PIKKs (Ki= 2.2, 3.9, 16, and >1 µM, respectively, against DNA-PK, PI 3-Kγ, ATM, and mTOR) and 50 other kinases. Shown to selectively inhibit ATR-dependent H2AX Ser139 & Chk1 Ser345 phosphorylation (complete inhibition at 10 µM in HT29 and HFL1 cultures) without affecting ATM- and DNA-PK-mediated H2AX or ATM-mediated Chk2 phosphorylation. Short-term (24 h) VE-821 treatment, either alone or in synergy with Cisplatin (Cat. No. 232120), results in reversible cytostatic growth arrest regardless of cellular ATM-p53 pathway activity, while cytotoxicity and Cisplatin synergism in cell death induction is reported to occur only upon long-term VE-821 exposure (≥72 h) in cultures with ATM-p53 pathway defects.
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1232410-49-9
      Chemical formulaC₁₈H₁₆N₄O₃S
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 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
      ReferencesPrevo, R., et al. 2012, Cancer Biol. Ther. 13, 1072; Pires, I.M., et al. 2012, Br. J. Cancer 107, 291; Reaper, P.M., et al. 2011, Nat. Chem. Biol. 7, 428.