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M8891 is an orally active, reversible, and brain-penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor (IC50: 54 nM; Ki: 4.33 nM). It inhibits the growth of primary endothelial cells and tumor cells, demonstrating both antiangiogenic and antitumoral activity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,520 | 6-8 weeks | |
50 mg | $1,980 | 6-8 weeks | |
100 mg | $2,500 | 6-8 weeks |
Description | M8891 is an orally active, reversible, and brain-penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor (IC50: 54 nM; Ki: 4.33 nM). It inhibits the growth of primary endothelial cells and tumor cells, demonstrating both antiangiogenic and antitumoral activity. |
Targets&IC50 | MetAP2:(ki)4.33 nM , MetAP2:54 nM |
In vitro | M8891 has an IC50 of 20 nM for HUVEC proliferation[1]. |
In vivo | 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]. |
Molecular Weight | 385.36 |
Formula | C20H17F2N3O3 |
Cas No. | 1464842-09-8 |
Relative Density. | 1.496 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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