TC Mps1 12

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

Research Areas >> Cancer

Signaling Pathways >> Cytoskeleton >> Mps1

Signaling Pathways >> Cell Cycle/DNA Damage >> Mps1

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]. Cell Viability Assay[1] Cell Line: 549 cells Concentration: Incubation Time: 72 hours Result: Inhibited the growth of cells in a dose-dependent manner and with an IC50 values of 0.84 μM.

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]. Animal Model: A549 mouse xenograft model[1] Dosage: 25 mg/kg, 50 mg/kg, 100 mg/kg Administration: Oral administration; once daily; for 19 days Result: Inhibited the growth of A549 cells in a dose-dependent manner. Animal Model: A549 mouse xenograft model (pharmacokinetic )[1] Dosage: 25 mg/kg Administration: Oral administration Result: Cmax = 3542 ng/mL, AUC = 6604 ng h/mL

[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.