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M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor(IC50 :54nM;Ki:4.33 nM).M8891 inhibits growth of primary endothelial cells as well as tumor cells and demonstrates antiangiogenic and antitumoral activity.
M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor(IC50 :54nM;Ki:4.33 nM).M8891 inhibits growth of primary endothelial cells as well as tumor cells and demonstrates antiangiogenic and antitumoral activity.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5 mg | ¥ 4,820 | 6-8周 | |
25 mg | ¥ 10,600 | 6-8周 | |
50 mg | ¥ 13,800 | 6-8周 | |
100 mg | ¥ 17,500 | 6-8周 |
产品描述 | M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor(IC50 :54nM;Ki:4.33 nM).M8891 inhibits growth of primary endothelial cells as well as tumor cells and demonstrates antiangiogenic and antitumoral activity. |
靶点活性 | MetAP2:(ki)4.33 nM , MetAP2:54 nM |
体外活性 | M8891 has an IC50 of 20 nM for HUVEC proliferation[1]. |
体内活性 | M8891 (iv;?0.2 mg/kg) shows low clearance (CL ~0.03-0.4 L/h/kg corresponding to ~1-6% of the liver blood-flow), small to medium volume of distribution (Vss ~0.23-1.3 L/kg), and medium to high oral bioavailability (F ~40-80%)[1].?M8891 (po; 20 mg/kg; once a day for 14 days) exhibits strong tumor growth inhibition[1]. |
分子量 | 385.36 |
分子式 | C20H17F2N3O3 |
CAS No. | 1464842-09-8 |
密度 | 1.496 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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