1609584-72-6
1609584-72-6 structure
- Name: Mps1-IN-3
- Chemical Name: Mps1-IN-3
- CAS Number: 1609584-72-6
- Molecular Formula: C26H31N7O4S
- Molecular Weight: 537.634
- Catalog: Signaling Pathways Cell Cycle/DNA Damage Mps1
- Create Date: 2018-06-22 06:03:44
- Modify Date: 2025-08-23 10:13:49
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Mps1-IN-3 is a potent and selective MPS1 kinase inhibitor, with an IC50 of 50 nM.
| Name | Mps1-IN-3 |
|---|---|
| Synonyms |
4-Piperidinol, 1-[3-methoxy-4-[[6-[[2-[(1-methylethyl)sulfonyl]phenyl]amino]-9H-purin-2-yl]amino]phenyl]-
1-{4-[(6-{[2-(Isopropylsulfonyl)phenyl]amino}-3H-purin-2-yl)amino]-3-methoxyphenyl}-4-piperidinol MFCD28053522 |
| Description | Mps1-IN-3 is a potent and selective MPS1 kinase inhibitor, with an IC50 of 50 nM. |
|---|---|
| Related Catalog | |
| Target |
Mps1:50 nM (IC50) |
| In Vitro | 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. Furthermore, Mps1-IN-3 (5 μM) sensitizes all glioblastoma cells (U251, U87, VU147 and GBM8) to 3 nM of vincristine[1]. |
| In Vivo | Mps1-IN-3 (2 mg/kg, i.v.) sensitizes glioblastoma cells to vincristine in murine tumor models, with prolonged survival and no toxicity[1]. |
| Animal Admin | 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, 0.5 mg/kg body weight vincristine in DMSO, 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 |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Molecular Formula | C26H31N7O4S |
| Molecular Weight | 537.634 |
| Exact Mass | 537.215820 |
| LogP | 0.57 |
| Index of Refraction | 1.677 |
| Storage condition | 2-8°C |