2. Metabolic Enzyme/Protease
  3. MetAP
  4. M8891

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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5 mg USD 580 In-stock
10 mg USD 980 In-stock
25 mg USD 1900 In-stock
50 mg USD 3200 In-stock
100 mg USD 5000 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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M8891 Related Antibodies

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  • Purity & Documentation

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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]
Cellular Effect
Cell Line Type Value Description References
HUVEC IC50
20 nM
Compound: 16; M8891
Inhibition of MetAP2 in HUVEC assessed as reduction in viability incubated for 3 days by CyQUANT Direct Cell proliferation assay
Inhibition of MetAP2 in HUVEC assessed as reduction in viability incubated for 3 days by CyQUANT Direct Cell proliferation assay
[PMID: 31725285]
In Vitro

M8891 has an IC50 of 20 nM for HUVEC proliferation[1].

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

M8891 Related Antibodies
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].

MedChemExpress (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%).
Clinical Trial
Molecular Weight

385.36

Formula

C20H17F2N3O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C([C@]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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 90 mg/mL (233.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.97% ee.: 99.25%

SDS (251 KB)

COA (249 KB) HNMR (182 KB) RP-HPLC (197 KB) NP-HPLC (310 KB) LCMS (143 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5950 mL 12.9749 mL 25.9498 mL 64.8744 mL
5 mM 0.5190 mL 2.5950 mL 5.1900 mL 12.9749 mL
10 mM 0.2595 mL 1.2975 mL 2.5950 mL 6.4874 mL
15 mM 0.1730 mL 0.8650 mL 1.7300 mL 4.3250 mL
20 mM 0.1297 mL 0.6487 mL 1.2975 mL 3.2437 mL
25 mM 0.1038 mL 0.5190 mL 1.0380 mL 2.5950 mL
30 mM 0.0865 mL 0.4325 mL 0.8650 mL 2.1625 mL
40 mM 0.0649 mL 0.3244 mL 0.6487 mL 1.6219 mL
50 mM 0.0519 mL 0.2595 mL 0.5190 mL 1.2975 mL
60 mM 0.0432 mL 0.2162 mL 0.4325 mL 1.0812 mL
80 mM 0.0324 mL 0.1622 mL 0.3244 mL 0.8109 mL
100 mM 0.0259 mL 0.1297 mL 0.2595 mL 0.6487 mL
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M8891 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

M88911464842-09-8M 8891M-8891MetAPMethionine AminopeptidaseReversiblebrainpenetrantMethionineAminopeptidase-2MetAP-2MetAP-1tumorantiangiogenicantitumoralInhibitorinhibitorinhibit

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