530391 MPS1 Inhibitor II, MPS1-IN-3 - Calbiochem

530391
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₆H₃₁N₇O₄S

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      5.30391.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell permeable, non-toxic compound with a purine core scaffold that acts as a highly potent inhibitor of monopolar spindle1 kinase (MPS1; IC50 = 50 nM). Displays good selectivity when screen against a panel of 450+ protein kinases. Reduces the levels of cyclin B that can be reversed by addition of proteasome inhibitor MG-132 (Cat. No. 474790). Inhibits SMAD2 phosphorylation and blocks the proliferation of U251 glioblastoma cells (IC50 = 5 µM). Increasingly sensitizes U251 cells to the action of vincristine (~ 3 nM) in vitro and in orthotopic mouse model of glioblastoma (2 mg/kg) leading to their prolonged survival.

          Please note that the molecular weight for this compound is batch-specific due to variable water content.
          Catalogue Number530391
          Brand Family Calbiochem®
          SynonymsMonopolar Spindle 1 Kinase Inhibitor
          References
          ReferencesTannous, B.A., et al. 2013. J. Natl. Cancer Inst. 105,1322.
          Product Information
          FormOff-white solid
          Hill FormulaC₂₆H₃₁N₇O₄S
          Chemical formulaC₂₆H₃₁N₇O₄S
          ReversibleY
          Applications
          Biological Information
          Primary TargetMPS1
          Primary Target IC<sub>50</sub>50 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
          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 3 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          MPS1 Inhibitor II, MPS1-IN-3 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Tannous, B.A., et al. 2013. J. Natl. Cancer Inst. 105,1322.
          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.

          Revision31-July-2014 JSW
          SynonymsMonopolar Spindle 1 Kinase Inhibitor
          DescriptionA cell permeable, non-toxic compound with a purine core scaffold that acts as a highly potent inhibitor of monopolar spindle1 kinase (MPS1; IC50 = 50 nM). Displays good selectivity when screen against a panel of 450+ protein kinases. Reduces the levels of cyclin B that can be reversed by addition of proteasome inhibitor MG-132 (Cat. No. 474790). Inhibits SMAD2 phosphorylation and blocks the proliferation of U251 glioblastoma cells (IC50 = 5 µM). Increasingly sensitizes U251 cells to the action of vincristine (~ 3 nM) in vitro and in orthotopic mouse model of glioblastoma (2 mg/kg) leading to their prolonged survival.
          FormOff-white solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₆H₃₁N₇O₄S
          Purity≥98% by HPLC
          SolubilityDMSO (25 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 Standard Handling
          ReferencesTannous, B.A., et al. 2013. J. Natl. Cancer Inst. 105,1322.