BAY-1217389CAS号: 1554458-53-5分子式: C27H24F5N5O3分子量: 561.503描述纯度储存/保存方法别名可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
BAY 1217389 is a potent, and selective inhibitor of the monopolar spindle 1 (MPS1) kinase with an IC50 value less than 10 nM. |
纯度 |
>98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
别名 |
BAY1217389
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可溶性/溶解性 |
DMSO :93 mg/mL (165.6 mM)
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生物活性 | |
靶点 |
Mps1
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In vitro(体外研究) |
In biochemical assays, the IC50 value of BAY 1217389 is 0.63±0.27 nmol/L. It shows high selectivity against other kinases and found to bind to PDGFRβ (300 nmol/L).
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In vivo(体内研究) |
In vivo, BAY 1217389 achieves moderate efficacy in monotherapy in tumor xenograft studies. Its blood clearance is found to be low in the tested species. Vss is high and terminal half-lives were long. BAY 1217389 is administered orally to female NMRI mouse (1 mg/kg) and male Wistar rat (0.5 mg/kg). Peak plasma concentrations are observed between 1.5 and 7 hours. Oral bioavailability is high in rat and moderate in mouse.
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分子结构图