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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      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
      Quality LevelMQ100
      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.