TC-Mps1-12 

TC-Mps1-12 is a potent and selective monopolar spindle 1 (Mps1) inhibitor, with an IC₅₀ of 6.4 nM^[1].

IC50: 6.4 nM (Mps1)^[1]

TC-Mps1-12 inhibits the growth of pMps1 cell lines with IC50 values of 131 nM in autophosphorylation assay^[1].
TC-Mps1-12 (72 hours) inhibits the growth of cells in a dose-dependent manner and with an IC₅₀ values of 0.84 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TC-Mps1-12 (25-100 mg/kg; p.o.; daily; for 19 days) inhibits the growth of A549 cells in a dose-dependent manner in vivo. At a dose of 100 mg/kg, TC-Mps1-12 exhibits 47% tumor growth inhibition without body weight loss^[1].
TC-Mps1-12 shows good PK properties with a Cmax of 3542 ng/mL and AUC of 6604 ng h/mL at an oral dose of 25 mg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

324.38

C₁₇H₂₀N₆O

1206170-62-8

Solid

White to off-white

N#CC1=C(N=C(NC2=CC=C(C(N)=O)C=C2)C=C1N)NC(C)(C)C

Room temperature in continental US; may vary elsewhere.

• [1]. Kusakabe K, et al. Diaminopyridine-based potent and selective mps1 kinase inhibitors binding to an unusual flipped-Peptide conformation. ACS Med Chem Lett. 2012 Jun 6;3(7):560-4.  [Content Brief]