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M8891

Catalog No. T11930   CAS 1464842-09-8

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.

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M8891 Chemical Structure
M8891, CAS 1464842-09-8
Pack Size Availability Price/USD Quantity
25 mg 6-8 weeks $ 1,520.00
50 mg 6-8 weeks $ 1,980.00
100 mg 6-8 weeks $ 2,500.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 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.
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

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.

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Keywords

M8891 1464842-09-8 Others M-8891 M 8891 inhibitor inhibit

 

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