219494 Cdk/CKI Inhibitor, (R)-DRF053 - CAS 1186647-87-9 - Calbiochem

219494
  
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      Overview

      Replacement Information

      Key Spec Table

      Empirical FormulaCAS #
      C₂₃H₂₇N₇O • H₂O1186647-87-9
      Description
      OverviewA cell-permeable ATP-binding pocket-targeting (R)-Roscovitine (Cat. Nos. 550360 & 550364) derivative that is more potent than Roscovitine in inhibiting CDK1,CDK5, and CK1 activity (IC50 = 220,80,14 vs. 350, 200, 2300 nM, respectively), while maintaining selectivity against GSK-3α/β (IC50 = 4.1 µM). The CDK/CK1 dual-specificity nature of (R)-DRF053 most likely accounts for its superior activity to that of (R)-Roscovitine against β40 production from APP-expressing N2A cells (90% vs. 50% inhibition wtih 100 µM respective compound).
      Catalogue Number219494
      Brand Family Calbiochem®
      Synonyms2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(3-(2-pyridyl)phenylamino)-9-isopropylpurine, hydrate
      References
      ReferencesOumata, N., et al. J. Med. Chem. 51, 5229.
      Bettayeb, K., et al. 2008. Oncogene 27, 5797.
      Product Information
      CAS number1186647-87-9
      FormPale yellow solid
      Hill FormulaC₂₃H₂₇N₇O • H₂O
      Chemical formulaC₂₃H₂₇N₇O • H₂O
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥95% 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 Ambient Temperature Only
      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

      Cdk/CKI Inhibitor, (R)-DRF053 - CAS 1186647-87-9 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Cdk/CKI Inhibitor, (R)-DRF053 - CAS 1186647-87-9 - Calbiochem Certificates of Analysis

      TitleLot Number
      219494

      References

      Reference overview
      Oumata, N., et al. J. Med. Chem. 51, 5229.
      Bettayeb, K., et al. 2008. Oncogene 27, 5797.
      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.

      Revision31-March-2011 RFH
      Synonyms2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(3-(2-pyridyl)phenylamino)-9-isopropylpurine, hydrate
      DescriptionA cell-permeable ATP-binding pocket-targeting (R)-Roscovitine (Cat. Nos. 550360 & 550364) derivative that is more potent than Roscovitine in inhibiting CDK1/CDK5/CK1 activity (IC50 = 220/80/14 vs. 350/200/2300 nM, respectively), while maintaining selectivity against GSK-3α/β (IC50 = 4.1 µM). The CDK/CK1 dual-specificity nature of (R)-DRF053 most likely accounts for its superior activity to that of (R)-Roscovitine against β40 production from APP-expressing N2A cells (90% vs. 50% inhibition wtih100 µM respective compound).
      FormPale yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1186647-87-9
      Chemical formulaC₂₃H₂₇N₇O • H₂O
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (50 mg/ml) or Ethanol (30 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
      ReferencesOumata, N., et al. J. Med. Chem. 51, 5229.
      Bettayeb, K., et al. 2008. Oncogene 27, 5797.