Mps1-IN-3 - CAS 1609584-72-6
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Not Intended for Therapeutic Use. For research use only.
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MPS1-IN-3 is a selective and potent MPS1 inhibitor with phenotypic consequences similar to those reported for published MPS1 inhibitors such as MPS1-IN-1, MPS1-IN-2, and AZD3146. Treatment with MPS1-IN-3 at 5 μM sensitized all glioblastoma cells to 3 nM of vincristine as measured by cell counts 11 days posttreatment. U251-FM cells were stereotactically injected into the brain of nude mice. Ten days postinjection, 2 mg/kg of MPS1-IN-3 and/or 0.5 mg/kg of vincristine were administered concomitantly by intravenous injections twice per week for 3 weeks.
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1.Effects of the selective MPS1 inhibitor MPS1-IN-3 on glioblastoma sensitivity to antimitotic drugs.
Tannous BA1, Kerami M, Van der Stoop PM, Kwiatkowski N, Wang J, Zhou W, Kessler AF, Lewandrowski G, Hiddingh L, Sol N, Lagerweij T, Wedekind L, Niers JM, Barazas M, Nilsson RJ, Geerts D, De Witt Hamer PC, Hagemann C, Vandertop WP, Van Tellingen O, Noske D J Natl Cancer Inst. 2013 Sep 4;105(17):1322-31. doi: 10.1093/jnci/djt168. Epub 2013 Aug 12.
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.
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CAS 1609584-72-6 Mps1-IN-3

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