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编 号:F070343
分子式:C17H20N6O
分子量:324.38
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1mg
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5mg
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10mg
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生物活性:
TC-Mps1-12 is a potent and selective monopolar spindle 1 (Mps1) inhibitor, with an IC50 of 6.4 nM.

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

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.
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