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217707 Cdc7/Cdk9 Inhibitor - CAS 845714-00-3 - Calbiochem

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217707
  
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      Overview

      Replacement Information

      Key Spec Table

      CAS #Empirical Formula
      845714-00-3C₁₂H₁₁N₃O
      Description
      Overview

      This product has been discontinued.



      A cell-permeable pyrrolopyridinone compound that acts as a potent, reversible, and ATP-competitive inhibitor of Cdc7 and Cdk9 (IC50 = 10 and 34 nM, respectively) with good selectivity over a panel of 31 other kinases, including GSK-3β, Cdk2, Cdk1, Cdk5, MK-2, Plk1, and Chk2 (IC50 = 0.22, 0.24, 0.25, 0.46, 0.47, 0.98, and 1.1 µM, respectively). Cellular treatment of PHA76749 results in a prevention of the activation of DNA replication origins without the inhibition of replication fork progression. Shown to inhibit the proliferation of 61 cell lines in vitro (IC50 ≤ 10 µM) and exhibit antitumor activity in both mice and rats in vivo.

      Catalogue Number217707
      Brand Family Calbiochem®
      Synonyms2-(Pyridin-4-yl)-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridinone, PHA-767491, Chk2 Inhibitor VI
      References
      ReferencesMontagnoli, A., et al. 2008. Nat Chem Biol. 4, 357.
      Vanotti, E., et al. 2008. J. Med. Chem. 51, 487.
      Anderson, D.R., et al. 2007. J. Med. Chem. 50, 2647.
      Product Information
      CAS number845714-00-3
      FormPink solid
      Hill FormulaC₁₂H₁₁N₃O
      Chemical formulaC₁₂H₁₁N₃O
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥90% 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
      217707 0

      Documentation

      Cdc7/Cdk9 Inhibitor - CAS 845714-00-3 - Calbiochem Certificates of Analysis

      TitleLot Number
      217707

      References

      Reference overview
      Montagnoli, A., et al. 2008. Nat Chem Biol. 4, 357.
      Vanotti, E., et al. 2008. J. Med. Chem. 51, 487.
      Anderson, D.R., et al. 2007. J. Med. Chem. 50, 2647.
      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.

      Revision05-April-2011 RFH
      Synonyms2-(Pyridin-4-yl)-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridinone, PHA-767491, Chk2 Inhibitor VI
      DescriptionA cell-permeable pyrrolopyridinone compound that acts as a potent, reversible, and ATP-competitive inhibitor of Cdc7 and Cdk9 (IC50 = 10 and 34 nM, respectively) with good selectivity over a panel of 31 other kinases, including GSK-3β, Cdk2, Cdk1, Cdk5, MK-2, Plk1, and Chk2 (IC50 = 0.22, 0.24, 0.25, 0.46, 0.47, 0.98, and 1.1 µM, respectively). Cellular treatment of PHA76749 results in a prevention of the activation of DNA replication origins without the inhibition of replication fork progression. Shown to inhibit the proliferation of 61 cell lines in vitro (IC50 ≤10 µM) and exhibit antitumor activity in both mice and rats in vivo.
      FormPink solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number845714-00-3
      Chemical formulaC₁₂H₁₁N₃O
      Structure formulaStructure formula
      Purity≥90% by HPLC
      SolubilityDMSO (25 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
      ReferencesMontagnoli, A., et al. 2008. Nat Chem Biol. 4, 357.
      Vanotti, E., et al. 2008. J. Med. Chem. 51, 487.
      Anderson, D.R., et al. 2007. J. Med. Chem. 50, 2647.