5.30391
MPS1 Inhibitor II, MPS1-IN-3
Synonym(s):
MPS1 Inhibitor II, MPS1-IN-3, Monopolar Spindle 1 Kinase Inhibitor
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About This Item
Empirical Formula (Hill Notation):
C26H31N7O4S
CAS Number:
Molecular Weight:
537.63
UNSPSC Code:
12352200
PubChem Substance ID:
Assay:
≥98% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
assay
≥98% (HPLC)
Quality Level
form
solid
potency
50 nM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
off-white
solubility
DMSO: 25 mg/mL
storage temp.
2-8°C
SMILES string
CC(C)S(=O)(=O)C1=CC=CC=C1NC2=NC(=NC3=C2NC=N3)NC4=C(C=C(C=C4)N5CCC(CC5)O)OC
General description
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.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
MPS1
MPS1
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Tannous, B.A., et al. 2013. J. Natl. Cancer Inst.105,1322.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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Global Trade Item Number
| SKU | GTIN |
|---|---|
| 5303910001 | 04055977260786 |