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

Zapnometinib (Synonyms: PD0184264; ATR-002)

Cat. No.: HY-139558 Purity: 99.63%
Handling Instructions

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

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5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
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25 mg USD 110 In-stock
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50 mg USD 205 In-stock
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100 mg USD 395 In-stock
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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].

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

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].

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.
Molecular Weight

409.55

Formula

C₁₃H₇ClF₂INO₂

CAS No.
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)

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
10 mM 0.2442 mL 1.2209 mL 2.4417 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 (5.08 mM); Clear solution

  • 2.

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

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

*All of the co-solvents are provided by MCE.
References
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Zapnometinib
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HY-139558
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