Name | 2-(2-chloro-4-iodoanilino)-3,4-difluorobenzoic acid |
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Synonyms | 2,8-dimercapto-6-hydroxypurine hydrate,1gr |
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]. |
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Related Catalog | |
Target |
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]. 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]. 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. |
References |
Molecular Formula | C13H7ClF2INO2 |
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Molecular Weight | 409.55 |
Exact Mass | 408.91800 |
PSA | 49.33000 |
LogP | 4.73760 |
~90% 303175-44-2 |
Literature: Davis, Edward M.; Nanninga, Thomas N.; Tjiong, Howie I.; Winkle, Derick D. Organic Process Research and Development, 2005 , vol. 9, # 6 p. 843 - 846 |
Precursor 2 | |
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DownStream 0 |