504972 ATR Inhibitor IV - CAS 1232410-49-10 - Calbiochem

504972
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₈H₁₆N₄O₃S 1232410-49-10

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      5.04972.0001
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          Glass bottle 10 mg
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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 number1232410-49-10
          FormYellow solid
          Hill FormulaC₁₈H₁₆N₄O₃S
          Chemical formulaC₁₈H₁₆N₄O₃S
          ReversibleY
          Structure formula ImageStructure formula Image
          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

          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.

          Revision09-December-2013 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 number1232410-49-10
          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.