Toggle Nav
Close
  • Menu
  • Setting

TC Mps1 12

Catalog No.
B7709
Mps1 inhibitor
Grouped product items
SizePriceStock Qty
10mg
$345.00
Ship with 5-10 days
50mg
$1,430.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

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.

Chemical Properties

Physical AppearanceWhite solid
StorageStore at -20°C
M.Wt324.38
Cas No.1206170-62-8
FormulaC17H20N6O
Solubility<32.44mg/ml in DMSO; <6.49mg/ml in ethanol
Chemical Name4-((4-amino-6-(tert-butylamino)-5-cyanopyridin-2-yl)amino)benzamide
SDFDownload SDF
Canonical SMILESCC(C)(NC1=C(C(N)=CC(NC2=CC=C(C(N)=O)C=C2)=N1)C#N)C
Shipping ConditionShip with blue ice, or upon other requests.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

TC Mps1 12