| Bioactivity | M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor with an IC50 of 54 nM and a Ki of 4.33 nM. M8891 does not inhibit MetAP-1 (IC50>10 µM)[1]. M8891 inhibits growth of primary endothelial cells as well as tumor cells and demonstrates antiangiogenic and antitumoral activity[2]. |
| Target | IC50: 54 nM (MetAP-2)Ki: 4.33 nM (MetAP-2) |
| Invitro | M8891 has an IC50 of 20 nM for HUVEC proliferation[1]. |
| In Vivo | M8891 (po; 20 mg/kg; once a day for 14 days) exhibits strong tumor growth inhibition[1]. 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]. Animal Model: |
| Name | M8891 |
| CAS | 1464842-09-8 |
| Formula | C20H17F2N3O3 |
| Molar Mass | 385.36 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| Reference | [1]. Heinrich T, et al. Identification of Methionine Aminopeptidase-2 (MetAP-2) Inhibitor M8891: A Clinical Compound for the Treatment of Cancer. J Med Chem. 2019 Dec 26;62(24):11119-11134. [2]. Manja Friese-Hamim, et al. Abstract 3075: Antitumor activity of M8891, a potent and reversible inhibitor of methionine aminopeptidase 2. |