Mps1-IN-3 hydrochloride

• CAT Number: I043591
• CAS Number: 2989453-29-2
• Molecular Formula: C26H32ClN7O4S
• Molecular Weight: 574.09
• Purity: ≥95%
• Synonyms: 1-[3-methoxy-4-[[6-(2-propan-2-ylsulfonylanilino)-7H-purin-2-yl]amino]phenyl]piperidin-4-ol;hydrochloride
• InChI: InChI=1S/C26H31N7O4S.ClH/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);1H
• InChIKey: BDKTZCBXQCCHRK-UHFFFAOYSA-N
• SMILES: CC(C)S(=O)(=O)C1=CC=CC=C1NC2=NC(=NC3=C2NC=N3)NC4=C(C=C(C=C4)N5CCC(CC5)O)OC.Cl

Mps1-IN-3 hydrochloride is a potent and selective Mps1 inhibitor with an IC50 value of 50 nM. Mps1-IN-3 hydrochloride can inhibit the proliferation of glioblastoma cells, and effectively sensitizes glioblastomas to Vincristine in orthotopic glioblastoma xenograft model[1].
Mps1-IN-3 hydrochloride (0.3-10 μM) inhibits the marker of mitotic cells cyclin B in a dose-dependent manner[1].
Mps1-IN-3 hydrochloride (2 μM) causes a dose-dependent escape from a checkpoint-mediated mitotic arrest[1].
Mps1-IN-3 hydrochloride (1-15 μM) inhibits the proliferation of U251 glioblastoma cells with an IC50 value of ~5 µM[1].
Mps1-IN-3 hydrochloride (2 mg/kg; IV, twice a week, for 3 weeks) effectively sensitizes glioblastomas to Vincristine in orthotopic glioblastoma xenograft models[1].

Reference

[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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