Chemical Structure : RMS-07
货号: PC-38336Not For Human Use, Lab Use Only.
RMS-07 (RMS 07) is the first potent, selective irreversible covalent inhibitor of Monopolar spindle kinase 1 (MPS1/TTK) with IC50 of 13 nM, Ki of 0.83 nM.
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RMS-07 (RMS 07) is the first potent, selective irreversible covalent inhibitor of Monopolar spindle kinase 1 (MPS1/TTK) with IC50 of 13 nM, Ki of 0.83 nM.
RMS-07 demonstrated intracellular target engagement with IC50 of 22.4 nM, shows a high selectivity against MAPKAPK2/3, FGFR4, p70S6Kβ (IC50>1 uM).
RMS-07 induced cell cycle arrest with a prolonged G2/M phase, downregulated cyclin B1, whereas it upregulated p53, p21, and phospho-γH2A.X, enhanced cleaved PARP levels; RMS-07 attenuates cancer cell proliferation.
RMS-07 and Navitoclax synergistically inhibit hepatocellular carcinoma cell proliferation.
分子量 | 604.759 | |
分子式 | C35H40N8O2 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Ricardo A M Serafim, et al. J Med Chem. 2022 Feb 15.
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