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

219494
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₃H₂₇N₇O • H₂O 1186647-87-9

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      219494-5MG
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          Glass bottle 5 mg
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          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 Image
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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 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.