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M8891 

Cat. No.: HY-133016
Handling Instructions

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). M8891 inhibits growth of primary endothelial cells as well as tumor cells and demonstrates antiangiogenic and antitumoral activity.

For research use only. We do not sell to patients.

M8891 Chemical Structure

M8891 Chemical Structure

CAS No. : 1464842-09-8

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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].

IC50 & 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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%).
Molecular Weight

385.36

Formula

C₂₀H₁₇F₂N₃O₃

CAS No.

1464842-09-8

SMILES

O=C([[email protected]]1(O)C(N(C2=CC3=C(NC=C3)C=C2)CC1)=O)NCC4=CC(F)=CC(F)=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (324.37 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5950 mL 12.9749 mL 25.9498 mL
5 mM 0.5190 mL 2.5950 mL 5.1900 mL
10 mM 0.2595 mL 1.2975 mL 2.5950 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.40 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.40 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.40 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

M8891M 8891M-8891OthersReversiblebrainpenetrantMethionineAminopeptidase-2MetAP-2MetAP-1tumorantiangiogenicantitumoralInhibitorinhibitorinhibit

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M8891
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HY-133016
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