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TC Mps1 12
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
TC Mps1 12图片
CAS NO:1206170-62-8
包装与价格：
包装价格(元)
10mg电议
50mg电议

产品介绍
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。
Cas No.1206170-62-8
化学名4-((4-amino-6-(tert-butylamino)-5-cyanopyridin-2-yl)amino)benzamide
Canonical SMILESCC(C)(NC1=C(C(N)=CC(NC2=CC=C(C(N)=O)C=C2)=N1)C#N)C
分子式C17H20N6O
分子量324.38
溶解度<32.44mg/ml in DMSO;<6.49mg/ml in ethanol
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.