TC Mps1 12

TC Mps1 12 是一种有效的选择性单极纺锤体 1 (Mps1) 抑制剂，IC50 为 6.4 nM。

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10mg

￥3600.00

2880.00

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50mg

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12070.00

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货号: ajci11696
CAS: 1206170-62-8
别名:
分子式: C17H20N6O
分子量: 324.38
纯度: >98%
溶解度: <32.44mg/ml in DMSO; <6.49mg/ml in ethanol
储存: Store at -20°C
库存: 现货

Background

Target: Monopolar spindle 1 (Mps1)

IC50: 6.4 nM

TC Mps1 12 is a potent and selective monopolar spindle 1 (Mps1) inhibitor with IC50 value of 6.4 nM [1]. Monopolar spindle 1 (Mps1), also known as TTK, plays a critical role in the spindle assembly checkpoint, centrosome duplication, and the maintenance of chromosomal stability. Mps1 is highly expressed in cancer cells and activated during mitosis. Therefore, Mps1 is a promising anticancer drug target [1].

In vitro: TC Mps1 12 displayed an excellent selectivity profile in a panel of 95 kinases, except for the Flt3 and Flt3 mutants (D835Y) [1]. TC Mps1 12 showed cellular inhibition of Mps1with an IC50 value of 131 nM in cell line that stably expresses FLAG-tagged Mps1. In addition, TC Mps1 12 inhibited the growth of A549 lung carcinoma cell lines with IC50 value of 0.84 μM [1].

In vivo: TC Mps1 12 (25 mg/kg, oral administration) treatment showed good pharmacokinetic (PK) properties with a Cmax of 3542 ng/mL and AUC of 6604 ng h/mL in mice [1]. Moreover, TC Mps1 12 (25 to 100 mg/kg, oral administration) dose-dependently inhibited the tumor growth of A549 cells without body weight loss in the mouse A549 xenograft model [1].

Reference:
1.? Kusakabe K, Ide N, Daigo Y, Itoh T, Higashino K, Okano Y, et al. Diaminopyridine-based potent and selective mps1 kinase inhibitors binding to an unusual flipped-Peptide conformation. ACS Med Chem Lett. 2012;3(7):560-4.