| Field | Specification |
|---|---|
| Target | |
| Alternative names | PD0184264; ATR-002 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C13H7ClF2INO2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Zapnometinib, also known as PD0184264 or ATR-002, is an active metabolite of CI-1040 and a MEK inhibitor with an IC50 of 5.7 nM. It exhibits antiviral activity against influenza virus as well as antibacterial activity[1][2][3]. It is supplied as an off-white to gray solid (C13H7ClF2INO2, MW 409.55) at 99.85% purity.
Physical & Chemical Properties
| CAS Number | 303175-44-2 |
|---|---|
| Molecular Formula | C13H7ClF2INO2 |
| Molecular Weight | 409.55 g/mol |
| Purity | 99.85% |
| Appearance | Solid |
| Color | Off-white to gray |
| SMILES | O=C(O)C1=CC=C(F)C(F)=C1NC2=CC=C(I)C=C2Cl |
| Target | MEK |
| Signaling Pathway | MAPK/ERK Pathway; Anti-infection |
| Solubility | In Vitro: DMSO: 62.5 mg/mL (152.61 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | 4°C, protect from light. In solvent: -80°C, 6 months; -20°C, 1 month (protect from light). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
MEK 5.7 nM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 62.5 mg/mL (152.61 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); protect from light; avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.08 mg/mL (5.08 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.08 mg/mL (5.08 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
Zapnometinib (0.1 nM-1 μM) inhibits MEK, with IC50s of 30.96 nM in A549 cells, 357 nM in MDCK cells, and 15 nM in human PBMCs[1]. In human PBMCs, Zapnometinib (100 μM; 4 h) inhibits phosphorylation of ERK1/2 induced by Ionomycin (PMA/I)[1]. Viral titers of the IV strains H1N1pdm09 and H3N2 are reduced by Zapnometinib (1-100 μM)[1].
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
After lethal H1N1pdm09 infection in mice, Zapnometinib (8.4-75 mg/kg/day; p.o. three times a day) lowers lung virus titers and improves survival[1]. At 150 mg/kg, Zapnometinib gives AUC values of 860.02 μg h/mL by the i.v. route and 1953.68 μg h/mL by the oral route in mice[1].
| 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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