1464842-09-8
1464842-09-8 structure
- Name: M8891
- Chemical Name: M8891
- CAS Number: 1464842-09-8
- Molecular Formula: C20H17F2N3O3
- Molecular Weight: 385.36
- Catalog: Research Areas Cancer
- Create Date: 2020-01-23 09:58:51
- Modify Date: 2025-08-27 17:04:13
-
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].
| Name | M8891 |
|---|
| Description | 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]. |
|---|---|
| Related Catalog | |
| Target |
IC50: 54 nM (MetAP-2)[1] Ki: 4.33 nM (MetAP-2)[1] |
| In Vitro | 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: Female CD-1 nude mice aged 6-7 weeks with human U87-MG glioblastoma[1] Dosage: 20 mg/kg Administration: Po; once a day for 14 days Result: Exhibited strong tumor growth inhibition. Animal Model: Rat, dog and monkey[1] Dosage: 0.2 mg/kg (Pharmacokinetic Analysis) Administration: IV Result: Showed 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%). |
| References |
| Molecular Formula | C20H17F2N3O3 |
|---|---|
| Molecular Weight | 385.36 |