Mps1-IN-3CAS# 1609584-72-6 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 1609584-72-6 | SDF | Download SDF |
| PubChem ID | 91885443 | Appearance | Powder |
| Formula | C26H31N7O4S | M.Wt | 537.63 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble in DMSO | ||
| Chemical Name | 1-[3-methoxy-4-[[6-(2-propan-2-ylsulfonylanilino)-7H-purin-2-yl]amino]phenyl]piperidin-4-ol | ||
| SMILES | CC(C)S(=O)(=O)C1=CC=CC=C1NC2=NC(=NC3=C2NC=N3)NC4=C(C=C(C=C4)N5CCC(CC5)O)OC | ||
| Standard InChIKey | OFRMASLPWOMYHN-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C26H31N7O4S/c1-16(2)38(35,36)22-7-5-4-6-20(22)29-25-23-24(28-15-27-23)31-26(32-25)30-19-9-8-17(14-21(19)37-3)33-12-10-18(34)11-13-33/h4-9,14-16,18,34H,10-13H2,1-3H3,(H3,27,28,29,30,31,32) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
Mps1-IN-3 Dilution Calculator
Mps1-IN-3 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.86 mL | 9.3001 mL | 18.6002 mL | 37.2003 mL | 46.5004 mL |
| 5 mM | 0.372 mL | 1.86 mL | 3.72 mL | 7.4401 mL | 9.3001 mL |
| 10 mM | 0.186 mL | 0.93 mL | 1.86 mL | 3.72 mL | 4.65 mL |
| 50 mM | 0.0372 mL | 0.186 mL | 0.372 mL | 0.744 mL | 0.93 mL |
| 100 mM | 0.0186 mL | 0.093 mL | 0.186 mL | 0.372 mL | 0.465 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Mps1-IN-3 is a potent and selective MPS1 kinase inhibitor, with an IC50 of 50 nM.
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].
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.
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Effects of the selective MPS1 inhibitor MPS1-IN-3 on glioblastoma sensitivity to antimitotic drugs.[Pubmed:23940287]
J Natl Cancer Inst. 2013 Sep 4;105(17):1322-31.
BACKGROUND: Glioblastomas exhibit a high level of chemotherapeutic resistance, including to the antimitotic agents vincristine and taxol. During the mitotic agent-induced arrest, glioblastoma cells are able to perform damage-control and self-repair to continue proliferation. Monopolar spindle 1 (MPS1/TTK) is a checkpoint kinase and a gatekeeper of the mitotic arrest. METHODS: We used glioblastoma cells to determine the expression of MPS1 and to determine the effects of MPS1 inhibition on mitotic errors and cell viability in combination with vincristine and taxol. The effect of MPS1 inhibition was assessed in different orthotopic glioblastoma mouse models (n = 3-7 mice/group). MPS1 expression levels were examined in relation to patient survival. RESULTS: Using publicly available gene expression data, we determined that MPS1 overexpression corresponds positively with tumor grade and negatively with patient survival (two-sided t test, P < .001). Patients with high MPS1 expression (n = 203) had a median and mean survival of 487 and 913 days (95% confidence intervals [CI] = 751 to 1075), respectively, and a 2-year survival rate of 35%, whereas patients with intermediate MPS1 expression (n = 140) had a median and mean survival of 858 and 1183 days (95% CI = 1177 to 1189), respectively, and a 2-year survival rate of 56%. We demonstrate that MPS1 inhibition by RNAi results in sensitization to antimitotic agents. We developed a selective small-molecule inhibitor of MPS1, Mps1-IN-3, which caused mitotic aberrancies in glioblastoma cells and, in combination with vincristine, induced mitotic checkpoint override, increased aneuploidy, and augmented cell death. Mps1-IN-3 sensitizes glioblastoma cells to vincristine in orthotopic mouse models (two-sided log-rank test, P < .01), resulting in prolonged survival without toxicity. CONCLUSIONS: Our results collectively demonstrate that MPS1, a putative therapeutic target in glioblastoma, can be selectively inhibited by Mps1-IN-3 sensitizing glioblastoma cells to antimitotic drugs.
