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

530391
  
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₆H₃₁N₇O₄S
Description
Overview

This product has been discontinued.



A 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
Global Trade Item Number
Catalogue Number GTIN
530391 0

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 Protect from light
+2°C to +8°C
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.