203882 CR8, (S)-Isomer - CAS 1084893-56-0 - Calbiochem

203882
  
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      Overview

      Replacement Information

      Key Spec Table

      Empirical FormulaCAS #
      C₂₄H₂₉N₇O1084893-56-0
      Description
      OverviewA cell-permeable (R)-DRF053 (Cat. No. 219494) analog that acts as an ATP-binding pocket-targeting CDK/CK1 dual-specific inhibitor (IC50 = 0.15, 0.080, 0.060, 0.12, 0.11, and 0.61 µM against CDK1/B, CDK2/A, CDK2/E, CDK5/p25, CDK9/T, and CK1δ/ε, respectively). Although (S)-CR8 displays in general similar kinase inhibitory profile as its (R)-enantiomer (Cat. No. 203881), it does exhibit more enhanced and reduced activity against, respectively, Dyrk1A (IC50 = 0.9 µM) and GSK-3α/β (IC50 ≥ 30 µM). Both (R)- and (S)-CR8 are much more effective than (R)-Roscovitine (Cat. Nos. 550360 and 550364) in apoptosis induction in cell cultures.
      Catalogue Number203882
      Brand Family Calbiochem®
      Synonyms2-(S)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurine, (S)-CR8
      References
      ReferencesBettayeb, K., et al. 2008. Oncogene 27, 5797.
      Product Information
      CAS number1084893-56-0
      FormOff-white solid
      Hill FormulaC₂₄H₂₉N₇O
      Chemical formulaC₂₄H₂₉N₇O
      Structure formula ImageStructure formula Image
      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 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

      SDS

      Title

      Safety Data Sheet (SDS) 

      Certificates of Analysis

      TitleLot Number
      203882

      References

      Reference overview
      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-(S)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurine, (S)-CR8
      DescriptionA cell-permeable (R)-DRF053 (Cat. No. 219494) analog that acts as an ATP-binding pocket-targeting CDK/CK1 dual-specific inhibitor (IC50 = 0.15, 0.080, 0.060, 0.12, 0.11, and 0.61 µM against CDK1/B, CDK2/A, CDK2/E, CDK5/p25, CDK9/T, and CK1δ/ε, respectively). Although (S)-CR8 displays in general similar kinase inhibitory profile as its (R)-enantiomer (Cat. No. 203881), it does exhibit more enhanced and reduced activity against, respectively, Dyrk1A (IC50 = 0.9 µM) and GSK-3α/β (IC50 ≥30 µM). Both (R)- & (S)-CR8 are much more effective than (R)-Roscovitine (Cat. Nos. 550360 & 550364) in apoptosis induction in cell cultures.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1084893-56-0
      Chemical formulaC₂₄H₂₉N₇O
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (35 mg/ml) or Ethanol (20 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
      ReferencesBettayeb, K., et al. 2008. Oncogene 27, 5797.