TC-Mps1-12 是一种高效、选择性的Mps1抑制剂，其IC50值为 6.4 nM。
| 生物活性 | TC-Mps1-12 is a potent and selectivemonopolar spindle 1 (Mps1)inhibitor, with anIC50of 6.4 nM[1]. |
| IC50& Target | |
体外研究
(In Vitro) | 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 IC50values 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 IC50values of 0.84 μM. |
|
体内研究
(In Vivo) | 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 |
|
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
