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203881 CR8, (R)-Isomer - CAS 294646-77-8 - Calbiochem

A cell-permeable (R)-DRF053 analog that acts as an ATP-binding pocket-targeting CDK/CK1 dual-specific inhibitor.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurine, (R)-CR8, Cdk7 Inhibitor VII

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      Overview

      Replacement Information

      Key Spec Table

      CAS #Empirical Formula
      294646-77-8C₂₄H₂₉N₇O
      Description
      OverviewA cell-permeable (R)-DRF053 (Cat. No. 219494) analog that acts as an ATP-binding pocket-targeting CDK/CK1 dual-specific inhibitor (IC50 = 0.09, 0.072, 0.041, 0.11, 1.10, 0.18, and 0.40 µM against CDK1/B, CDK2/A, CDK2/E, CDK5/p25, CDK7/H, CDK9/T, and CK1δ/ε, respectively). As is the case with (R)-DRF053, (R)-CR8 inhibits CDK/CK1 more effectively than (R)-Roscovitine (Cat. Nos. 550360 & 550364), while maintaining similar selectivity profile over other types of kinases (IC50 = 3.6, 3.6, and 12.0 µM against Dyrk1A, Erk2, and GSK-3α/β, respectively). Both the (R)-CR8 and (S)-enantiomer (Cat. No. 203882) are much more effective than (R)-Roscovitine in apoptosis induction in cell cultures.
      Catalogue Number203881
      Brand Family Calbiochem®
      Synonyms2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurine, (R)-CR8, Cdk7 Inhibitor VII
      References
      ReferencesOumata, N., et al. J. Med. Chem. 51, 5229.
      Bettayeb, K., et al. 2008. Oncogene 27, 5797.
      Product Information
      CAS number294646-77-8
      FormOff-white solid
      Hill FormulaC₂₄H₂₉N₇O
      Chemical formulaC₂₄H₂₉N₇O
      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 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
      Global Trade Item Number
      Catalogue Number GTIN
      203881 0

      Documentation

      Required Licenses

      Title
      PRODUCTO REGULADO POR LA SECRETARÍA DE SALUD

      CR8, (R)-Isomer - CAS 294646-77-8 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      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-(4-(2-pyridyl)benzyl)-9-isopropylpurine, (R)-CR8, Cdk7 Inhibitor VII
      DescriptionA cell-permeable (R)-DRF053 (Cat. No. 219494) analog that acts as an ATP-binding pocket-targeting CDK/CK1 dual-specific inhibitor (IC50 = 0.09, 0.072, 0.041, 0.11, 1.10, 0.18, and 0.40 µM against CDK1/B, CDK2/A, CDK2/E, CDK5/p25, CDK7/H, CDK9/T, and CK1δ/ε, respectively). As is the case with (R)-DRF053, (R)-CR8 inhibits CDK/CK1 more effectively than (R)-Roscovitine (Cat. Nos. 550360 & 550364), while maintaining similar selectivity profile over other types of kinases (IC50 = 3.6, 3.6, and 12.0 µM against Dyrk1A, Erk2, and GSK-3α/β, respectively). Both (R)-CR8 & its (S)-enantiomer (Cat. No. 203882) are much more effective than (R)-Roscovitine in apoptosis induction in cell cultures.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number294646-77-8
      Chemical formulaC₂₄H₂₉N₇O
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (50 mg/ml) or Ethanol (15 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      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.