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118510 ATR Kinase Inhibitor II - Calbiochem

118510
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118510-10MG
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      Description
      OverviewA cell-permeable aminopyrazinyl-sulfone compound that acts as a potent, reversible and ATP-competitive inhibitor of ATR kinase (IC50 = 12 nM; Ki = 6 nM) with excellent selectivity over ATM, DNA-PK (IC50 > 8 µM) and in a 50-kinase panel (% inhibition at 2 µM = 59, 57, 55, 52, 43 and 42 for AMPK, Lck, RIPK2, Ret, IKKα and FGFR3, respectively). Shown to block pH2AX-Ser139 (IC50 = 420 nM in hydroxyurea treated HT29 cells) and preferentially enhance cisplatin (Cat. No. 232120) cytotoxicity against tumor cells over normal cells by ~7-fold at 620 nM.
      Catalogue Number118510
      Brand Family Calbiochem®
      Synonyms3-Amino-6-(4-((1-(dimethylamino)propan-2-yl)sulfonyl)-phenyl)-N-phenylpyrazine-2-carboxamide
      References
      ReferencesCharrier, J.D., et al. 2011. J. Med. Chem. 54, 2320.
      Product Information
      FormYellow powder
      Hill FormulaC₂₂H₂₅N₅O₃S
      Chemical formulaC₂₂H₂₅N₅O₃S
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥97% by HPLC
      Physicochemical Information
      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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      ATR Kinase Inhibitor II - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Charrier, J.D., et al. 2011. J. Med. Chem. 54, 2320.
      Fiche technique

      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-August-2013 JSW
      Synonyms3-Amino-6-(4-((1-(dimethylamino)propan-2-yl)sulfonyl)-phenyl)-N-phenylpyrazine-2-carboxamide
      DescriptionA cell-permeable aminopyrazinyl-sulfone compound that acts as a potent, reversible and ATP-competitive inhibitor of ATR kinase (IC50 = 12 nM; Ki = 6 nM) with excellent selectivity over ATM, DNA-PK (IC50 > 8 µM) and in a 50-kinase panel (% inhibition at 2 µM = 59, 57, 55, 52, 43 and 42 for AMPK, Lck, RIPK2, Ret, IKKα and FGFR3, respectively). Shown to block pH2AX-Ser139 (IC50 = 420 nM in hydroxyurea treated HT29 cells) and preferentially enhance cisplatin (Cat. No. 232120) cytotoxicity against tumor cells over normal cells by ~7-fold at 620 nM.
      FormYellow powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₂H₂₅N₅O₃S
      Structure formulaStructure formula
      Purity≥97% 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 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesCharrier, J.D., et al. 2011. J. Med. Chem. 54, 2320.