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

Polo-Like Kinase Inhibitor VI, NMS-P937, CAS 1034616-18-6, is a cell-permeable, highly potent, reversible, and ATP-competitive inhibitor of polo-like kinase 1 (Plk1; IC₅₀ = 2 nM).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: PLK1 Inhibitor II, NMS P937, NMS-1286937

Primary Target: Plk1
533380
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Overview

Replacement Information

Key Specifications Table

Empirical FormulaCAS #
C₂₄H₂₇F₃N₈O₃ 1034616-18-6

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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
      Quality LevelMQ100
      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.