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

445821
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      Overview

      Replacement Information

      Key Spec Table

      Empirical FormulaCAS #
      C₁₂H₁₁N₅O954143-48-7

      Pricing & Availability

      Catalogue NumberAvailability Packaging Qty/Pack Price Quantity
      445821-5MG
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          Plastic ampoule 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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          445821

          References

          Reference overview
          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.