GLPBio

Mps1-IN-3

Catalog No.: GC36651Purity:>99.00%
Mps1-IN-3 is a potent and selective MPS1 kinase inhibitor, with an IC50 of 50 nM.

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Mps1-IN-3
Cas No.: 1609584-72-6
10mM (in 1mL DMSO)In Stock
$75.00
1
5mgIn Stock
$63.00
1
10mgIn Stock
$97.00
1
25mgIn Stock
$195.00
1
50mgIn Stock
$311.00
1
100mgIn Stock
$495.00
1

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Description

Mps1-IN-3 is a potent and selective MPS1 kinase inhibitor, with an IC50 of 50 nM. Mps1|50 nM (IC50)

Mps1-IN-3 is a potent MPS1 kinase inhibitor, with an IC50 of 50 nM. Mps1-IN-3 inhibits the proliferation of U251 glioblastoma cells with an IC50 of appr 5 µM. Mps1-IN-3 (2 μM) can completely abrogates checkpoint[1].

Mps1-IN-3 (2 mg/kg, i.v.) sensitizes glioblastoma cells in murine tumor models, with prolonged survival and no toxicity[1].

[1]. Tannous BA, et al. Effects of the selective MPS1 inhibitor MPS1-IN-3 on glioblastoma sensitivity to antimitotic drugs. J Natl Cancer Inst. 2013 Sep 4;105(17):1322-31.

Protocol

Animal experiment:

Mice[1]Six-week old athymic female nude mice weighing about 25 g are stereotactically injected with 1 × 106 U251-FM-shCTRL or shMPS1 cells, or U251-FM, or 3 × 105 GBM8-FM cells (in 10 and 4 μL PBS, respectively) using a stereotactic instrument after drilling a small hole in the cranium of the mice. For the U251-FM-shRNA experiment, a minimum of 3 mice per group is used, and for the U251-FM and GBM8-FM cells, at least 5 mice per group are used. Tumor growth is monitored by Fluc bioluminescence imaging after injection of 150 μL D-luciferin (50 mg/mL) and imaging 10 min later for luciferase-mediated photon activity using the IVIS Lumina imaging system for the U251-FM model and the IVIS Spectrum for the GBM8-FM model. When tumors reach a size around 107 radiance for the U251 model and 5 × 105 radiance for the GBM8 model, mice are intravenously injected with vehicle, and/or 2 mg/kg MPS1-IN-3 in 20% hydroxypropyl-beta-cyclodextrin (HPbetaCD), twice/week over three weeks. Tumor volume is monitored weekly by Fluc imaging[1].

References:

[1]. Tannous BA, et al. Effects of the selective MPS1 inhibitor MPS1-IN-3 on glioblastoma sensitivity to antimitotic drugs. J Natl Cancer Inst. 2013 Sep 4;105(17):1322-31.

Product Documents

Purity:>99.00%Appearance:A solid

Chemical Properties

CAS No.
1609584-72-6
SMILES
O=S(C1=C(NC2=NC(NC3=CC=C(N4CCC(O)CC4)C=C3OC)=NC5=C2N=CN5)C=CC=C1)(C(C)C)=O
Molecular Formula
C26H31N7O4S
Molecular Weight
537.63
Solubility
Soluble in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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