445821 Meriolin 3 - CAS 954143-48-7 - Calbiochem

445821
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Empirical FormulaCAS #
C₁₂H₁₁N₅O 954143-48-7

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445821-5MG
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      Ampulka plastikowa 5 mg
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      Description
      OverviewA cell-permeable, ATP site-targeting azaindolopyrimidine compound that is reported to inhibit the kinase activity of CDK9/cyclin T, CDK2/cyclin A, CDK1/cyclin B, CDK5/p25 (IC50 = 6, 11, 170, 170 nM, respectively), DYRK1A, CKIδ/ε, GSK-3α/β (IC50 = 29, 200, and 230 nM, respectively), as well as CDK3/cyclin E, CDK4/cyclin D1, CDK6/cyclin D1, CDK7/cyclin H, and FLT3 (IC50 <400 nM), while showing much reduced activity agasint 21 other kinases (IC50 >1 µM). Shown to effectively inhibit cellular CDK substrates phosphorylation and induce apoptosis in SH-SY5Y neuroblastoma cultures (Effective conc. 0.3 to 1 µM) in vitro and retard A4573- and LS174T-derived tumor growths in mice in vivo (1 to 5 mg/kg/day, i.p.). Cell viability tests reveal that Meriolin 3 selectively affects the viability of a panel of 8 cancer lines (IC50 ≤380 nM) in comparison to normal human foreskin fibroblasts (IC50 = 8 µM).
      Catalogue Number445821
      Brand Family Calbiochem®
      Synonyms3-((2-Amino)pyrimidin-4-yl)-4-methoxy-1H-pyrrolo[2,3-b]pyridine, Cdk7 Inhibitor VI
      References
      ReferencesEchalier, A., et al. 2008. J. Med. Chem. 51, 737.
      Bettayeb, K., et al. 2007. Cancer Res. 67, 8325.
      Product Information
      CAS number954143-48-7
      FormYellow solid
      Hill FormulaC₁₂H₁₁N₅O
      Chemical formulaC₁₂H₁₁N₅O
      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 Regulatory Review
      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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Meriolin 3 - CAS 954143-48-7 - Calbiochem MSDS

      Title

      Safety Data Sheet (SDS) 

      Meriolin 3 - CAS 954143-48-7 - Calbiochem Certificates of Analysis

      TitleLot Number
      445821

      References

      Przegląd literatury
      Echalier, A., et al. 2008. J. Med. Chem. 51, 737.
      Bettayeb, K., et al. 2007. Cancer Res. 67, 8325.
      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.

      Revision13-April-2011 RFH
      Synonyms3-((2-Amino)pyrimidin-4-yl)-4-methoxy-1H-pyrrolo[2,3-b]pyridine, Cdk7 Inhibitor VI
      DescriptionA cell-permeable, ATP site-targeting azaindolopyrimidine compound that is reported to inhibit the kinase activity of CDK9/cyclin T, CDK2/cyclin A, CDK1/cyclin B, CDK5/p25 (IC50 = 6, 11, 170, 170 nM, respectively), DYRK1A, CKIδ/ε, GSK-3α/β (IC50 = 29, 200, and 230 nM, respectively), as well as CDK3/cyclin E, CDK4/cyclin D1, CDK6/cyclin D1, CDK7/cyclin H, and FLT3 (IC50 <400 nM), while showing much reduced activity agasint 21 other kinases (IC50 >1 µM). Shown to effectively inhibit cellular CDK substrates phosphorylation and induce apoptosis in SH-SY5Y neuroblastoma cultures (Effective conc. 0.3 to 1 µM) in vitro and retard A4573- and LS174T-derived tumor growths in mice in vivo (1 to 5 mg/kg/day, i.p.). Cell viability tests reveal that Meriolin 3 selectively affects the viability of a panel of 8 cancer lines (IC50 ≤380 nM) in comparison to normal human foreskin fibroblasts (IC50 = 8 µM).
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number954143-48-7
      Chemical formulaC₁₂H₁₁N₅O
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (50 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 3 months at -20°C.
      Toxicity Regulatory Review
      ReferencesEchalier, A., et al. 2008. J. Med. Chem. 51, 737.
      Bettayeb, K., et al. 2007. Cancer Res. 67, 8325.