533380 Polo-like Kinase Inhibitor VI, NMS-P937 - CAS 1034616-18-6 - Calbiochem

533380
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₄H₂₇F₃N₈O₃ 1034616-18-6

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      5.33380.0001
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          Glass bottle 5 mg
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          Description
          OverviewA cell-permeable, orally bioavailable, dihydropyrazoloquinazoline based compound that acts as a highly potent, reversible, and ATP-competitive inhibitor of polo-like kinase 1 (Plk1; IC50 = 2 nM). Displays excellent selectivity over Plk2 and Plk3 (IC50 > 10 µM). At higher concentrations affect the activities of fms-like tyrosine kinase (Flt3), maternal embryonic leucine zipper kinase (MELK), and casein kinase 2 (IC50 = 510, 744 and 826 nM, respectively). Preferentially blocks cell cycle at G2/M phase and induces apoptosis in cancer cells (IC50 = 42 nM in A2780 human ovarian carcinoma cells). Shown to suppress the growth of HCT116 colon adenocarcinoma cells xenografted in CD1 nu/nu mice (45 mg/kg, b.i.d). Also exhibits good potency on taxol (Cat. No. 580555) resistant tumor cells (IC50 = 65 and 62 nM for A2780 and 1A9 PTX ovarian adenocarcinoma cells, respectively). Displays desirable pharmacokinetic properties with t1/2 = 0.9 h; AUC = 8.7 µM/h; clearance = 2.36 L/h/kg (10 mg/kg, i.v.).

          Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
          Catalogue Number533380
          Brand Family Calbiochem®
          SynonymsPLK1 Inhibitor II, NMS P937, NMS-1286937
          References
          ReferencesCasolaro, A., et al. 2013. PLoS One 8, e58424.
          Valsasina, B., et al. 2012. Mol. Cancer Ther.11, 1006.
          Beria, I., et al. 2011. Bioorg. Med. Chem. Lett. 21, 2969.
          Product Information
          CAS number1034616-18-6
          FormPale yellow solid
          Hill FormulaC₂₄H₂₇F₃N₈O₃
          Chemical formulaC₂₄H₂₇F₃N₈O₃
          ReversibleY
          Applications
          Biological Information
          Primary TargetPlk1
          Primary Target IC<sub>50</sub>2 nM
          Purity≥98% by HPLC
          Physicochemical Information
          Cell permeableY
          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

          References

          Reference overview
          Casolaro, A., et al. 2013. PLoS One 8, e58424.
          Valsasina, B., et al. 2012. Mol. Cancer Ther.11, 1006.
          Beria, I., et al. 2011. Bioorg. Med. Chem. Lett. 21, 2969.
          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.

          Revision20-November-2015 JSW
          SynonymsPLK1 Inhibitor II, NMS P937, NMS-1286937
          DescriptionA cell-permeable, orally bioavailable, dihydropyrazoloquinazoline based compound that acts as a highly potent, reversible, and ATP-competitive inhibitor of polo-like kinase 1 (Plk1; IC50 = 2 nM). Displays excellent selectivity over Plk2 and Plk3 (IC50 > 10 µM). At higher concentrations affect the activities of fms-like tyrosine kinase (Flt3), maternal embryonic leucine zipper kinase (MELK), and casein kinase 2 (IC50 = 510, 744 and 826 nM, respectively). Preferentially blocks cell cycle at G2/M phase and induces apoptosis in cancer cells (IC50 = 42 nM in A2780 human ovarian carcinoma cells). Shown to suppress the growth of HCT116 colon adenocarcinoma cells xenografted in CD1 nu/nu mice (45 mg/kg, b.i.d). Also exhibits good potency on taxol (Cat. No. 580555) resistant tumor cells (IC50 = 65 and 62 nM for A2780 and 1A9 PTX ovarian adenocarcinoma cells, respectively). Displays desirable pharmacokinetic properties with t1/2 = 0.9 h; AUC = 8.7 µM/h; clearance = 2.36 L/h/kg (10 mg/kg, i.v.).
          FormPale yellow solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number1034616-18-6
          Chemical formulaC₂₄H₂₇F₃N₈O₃
          Purity≥98% by HPLC
          SolubilityDMSO (10 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
          ReferencesCasolaro, A., et al. 2013. PLoS One 8, e58424.
          Valsasina, B., et al. 2012. Mol. Cancer Ther.11, 1006.
          Beria, I., et al. 2011. Bioorg. Med. Chem. Lett. 21, 2969.