GLPBio

Mps1-IN-3

Catalog No.: GC36651Purity:>99.00%
Mps1-IN-3 es un potente y selectivo inhibidor de la cinasa MPS1, con una IC50 de 50 nM.

Los productos son exclusivamente para uso en investigación. No aptos para uso humano. No vendemos a pacientes.


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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    Nature
    641, 529–536 (2025)
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    628, 630–638 (2024)
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    632, 686–694 (2024)
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    618, 1017–1023 (2023)
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    Nature
    610, 366–372 (2022)
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    Cell
    187(9):2288-2304 (2024)
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    Cell
    183(7):1867-1883 (2020)
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    388(6745) (2025)
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    387(6734) (2025)
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    35, 97–116 (2025)
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    34, 683–706 (2024)
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    33, 273–287 (2023)
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    33, 546–561 (2023)
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    31, 1291–1307 (2021)

Descripción (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.

Protocolo (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.

Documentos del producto (Product Documents)

Purity:>99.00%Appearance:A solid

Propiedades químicas (Chemical Properties)

N.º CAS
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
Fórmula molecular
C26H31N7O4S
Peso molecular
537.63
Solubilidad
Soluble in DMSO
Almacenamiento
Store at -20°C
Consejos generales
Seleccione un disolvente adecuado según los datos de solubilidad del producto. Una vez preparada, divida la solución madre en alícuotas para evitar ciclos repetidos de congelación y descongelación.
Utilice las soluciones madre en un plazo de 6 meses si se conservan a -80°C, o de 1 mes si se conservan a -20°C.
Para mejorar la solubilidad, caliente el tubo a 37°C y soníquelo durante un periodo adecuado.
Condiciones de envío
Las muestras de evaluación se envían con acumuladores de frío. Los demás tamaños se envían a temperatura ambiente o, previa solicitud, con acumuladores de frío.

Calculadoras (Calculators)Molaridad / Dilución / Peso molecular / Conversión de unidades / Formulación in vivo / Solubilidad

g/mol

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