For research use only. Not for therapeutic Use.
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].
M8891 has an IC50 of 20 nM for HUVEC proliferation[1].
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].
| Catalog Number | I017367 |
| CAS Number | 1464842-09-8 |
| Synonyms | (3S)-N-[(3,5-difluorophenyl)methyl]-3-hydroxy-1-(1H-indol-5-yl)-2-oxopyrrolidine-3-carboxamide |
| Molecular Formula | C20H17F2N3O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C20H17F2N3O3/c21-14-7-12(8-15(22)10-14)11-24-18(26)20(28)4-6-25(19(20)27)16-1-2-17-13(9-16)3-5-23-17/h1-3,5,7-10,23,28H,4,6,11H2,(H,24,26)/t20-/m0/s1 |
| InChIKey | WVGGJQVCOTYFPV-FQEVSTJZSA-N |
| SMILES | C1CN(C(=O)C1(C(=O)NCC2=CC(=CC(=C2)F)F)O)C3=CC4=C(C=C3)NC=C4 |
| 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. |
