| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
MEK 5.7 nM (IC50)
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|---|---|
| ln Vitro |
In A549, MDCK cells, and human PBMC, zapnometinib (0.1 nM-1 μM) suppresses MEK with IC50s of 30.96 nM, 357 nM, and 15 nM, respectively[1]. In human PBMC, zapnometinib (100 μM; 4 hours) suppresses the phosphorylation of ERK1/2 caused by ionomycin (PMA/I) [1]. H3N2 and IV H1N1pdm09 virus titers are decreased by zapnometinib (1-100 μM) [1].
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| ln Vivo |
Zapnometinib (8.4–75 mg/kg/day; orally administered three times daily) decreases lung virus titers and increases mice survival following a fatal H1N1pdm09 infection [1]. Zapnometinib (150 mg/kg) administered intravenously or orally to mice resulted in AUC values of 860.02 and 1953.68 μg?h/mL, respectively [1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: human PBMCs Tested Concentrations: 100 μM Incubation Duration: 4 h Experimental Results: Inhibited the Ionomycin (PMA/I )-increased pERK1/2. |
| Animal Protocol |
Animal/Disease Models: Female C57BL/6 mice (8 weeks; 21-24 g) were infected with H1N1pdm09[1]
Doses: 8.4, 25, 75 mg/ kg/day (2.8, 8.4, 25 mg/kg) Route of Administration: Po three times a day Experimental Results: Dramatically diminished the virus titer at the dose of either 75 mg/kg/day or 25 mg/kg/day. |
| References |
[1]. Laure M, et, al. Antiviral efficacy against influenza virus and pharmacokinetic analysis of a novel MEK-inhibitor, ATR-002, in cell culture and in the mouse model. Antiviral Res. 2020 Jun;178:104806.
[2]. Hamza H, et, al. Improved in vitro Efficacy of Baloxavir Marboxil Against Influenza A Virus Infection by Combination Treatment With the MEK Inhibitor ATR-002. Front Microbiol. 2021 Feb 12;12:611958. [3]. Bruchhagen C, et, al. Metabolic conversion of CI-1040 turns a cellular MEK-inhibitor into an antibacterial compound. Sci Rep. 2018 Jun 14;8(1):9114. |
| Molecular Formula |
C13H7CLF2INO2
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|---|---|
| Molecular Weight |
409.55
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| CAS # |
303175-44-2
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| SMILES |
ClC1C=C(I)C=CC=1NC1C(F)=C(F)C=CC=1C(O)=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 62.5 mg/mL (152.61 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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