2. MAPK/ERK Pathway Anti-infection
  3. MEK Influenza Virus Bacterial
  4. Zapnometinib

Zapnometinib  (Synonyms: PD0184264; ATR-002)

Cat. No.: HY-139558 Purity: 99.85%
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Zapnometinib (PD0184264), an active metabolite of CI-1040, is a MEK inhibitor, with an IC50 of 5.7 nM. Zapnometinib exhibits antiviral activity against influenza virus and antibacterial activities.

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

Zapnometinib Chemical Structure

Zapnometinib Chemical Structure

CAS No. : 303175-44-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 55 In-stock
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Solid
5 mg USD 50 In-stock
10 mg USD 75 In-stock
25 mg USD 90 In-stock
50 mg USD 170 In-stock
100 mg USD 330 In-stock
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Based on 1 publication(s) in Google Scholar

Zapnometinib Related Antibodies

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Description

Zapnometinib (PD0184264), an active metabolite of CI-1040, is a MEK inhibitor, with an IC50 of 5.7 nM. Zapnometinib exhibits antiviral activity against influenza virus and antibacterial activities[1][2][3].

IC50 & Target[1]

MEK

5.7 nM (IC50)

In Vitro

Zapnometinib (0.1 nM-1 μM) inhibits MEK, with IC50s of 30.96 nM, 357 nM, and 15 nM in cell free kinase assay, A549, MDCK cells and human PBMCs[1].
Zapnometinib (100 μM; 4 h) inhibits the Ionomycin (PMA/I)-induced phosphorylation of ERK1/2 in human PBMCs[1].
Zapnometinib (1-100 μM) reduces the viral titers of the IV H1N1pdm09, H3N2[1].

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

Zapnometinib Related Antibodies

Western Blot Analysis[1]

Cell Line: human PBMCs
Concentration: 100 μM
Incubation Time: 4 h
Result: Inhibited the Ionomycin (PMA/I)-increased pERK1/2.
In Vivo

Zapnometinib (8.4-75 mg/kg/day; three times a day p.o.) reduces the lung virus titers and enhances survival of mice after lethal H1N1pdm09 infection[1].
Zapnometinib (150 mg/kg) exhibits AUC values of 860.02 and 1953.68 μg•h/mL in mice by i.v. or oral route, respectively[1].

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

Animal Model: Female C57BL/6 mice (8 weeks; 21-24 g) were infected with H1N1pdm09[1]
Dosage: 8.4, 25, 75 mg/kg/day (2.8, 8.4, 25 mg/kg)
Administration: P.o. three times a day
Result: Significantly reduced the virus titer at the dose of either 75 mg/kg/day or 25 mg/kg/day.
Clinical Trial
Molecular Weight

409.55

Formula

C13H7ClF2INO2
CAS No.
Appearance

Solid

Color

Off-white to gray

SMILES

O=C(O)C1=CC=C(F)C(F)=C1NC2=CC=C(I)C=C2Cl
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 : 62.5 mg/mL (152.61 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 2.4417 mL 12.2085 mL 24.4170 mL
5 mM 0.4883 mL 2.4417 mL 4.8834 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.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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 (5.08 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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (5.08 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 99.85%

COA (249 KB) LCMS (89 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 2.4417 mL 12.2085 mL 24.4170 mL 61.0426 mL
5 mM 0.4883 mL 2.4417 mL 4.8834 mL 12.2085 mL
10 mM 0.2442 mL 1.2209 mL 2.4417 mL 6.1043 mL
15 mM 0.1628 mL 0.8139 mL 1.6278 mL 4.0695 mL
20 mM 0.1221 mL 0.6104 mL 1.2209 mL 3.0521 mL
25 mM 0.0977 mL 0.4883 mL 0.9767 mL 2.4417 mL
30 mM 0.0814 mL 0.4070 mL 0.8139 mL 2.0348 mL
40 mM 0.0610 mL 0.3052 mL 0.6104 mL 1.5261 mL
50 mM 0.0488 mL 0.2442 mL 0.4883 mL 1.2209 mL
60 mM 0.0407 mL 0.2035 mL 0.4070 mL 1.0174 mL
80 mM 0.0305 mL 0.1526 mL 0.3052 mL 0.7630 mL
100 mM 0.0244 mL 0.1221 mL 0.2442 mL 0.6104 mL
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Zapnometinib 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:

Zapnometinib303175-44-2PD0184264 ATR-002PD 0184264PD-0184264ATR002ATR 002ATR-002MEKInfluenza VirusBacterialMitogen-activated protein kinase kinaseMAPKKMAP2KCI-1040antiviralinfluenzavirusantibacterialInhibitorinhibitorinhibit

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