TC-Mps1-12 is a potent and selective monopolar spindle 1 (Mps1) inhibitor, with an IC50 of 6.4 nM.
体外研究
TC-Mps1-12 inhibits the growth of pMps1 cell lines with IC50 values of 131 nM in autophosphorylation assay.
TC-Mps1-12 (72 hours) inhibits the growth of cells in a dose-dependent manner and with an IC50 values of 0.84 μM.
Cell Viability Assay
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.
体内研究
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.
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.
Animal Model:
A549 mouse xenograft model
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 )
Dosage:
25 mg/kg
Administration:
Oral administration
Result:
Cmax = 3542 ng/mL, AUC = 6604 ng h/mL
分子式
C17H20N6O
分子量
324.38
CAS号
1206170-62-8
运输条件
Room temperature in continental US; may vary elsewhere.