zapnometinib

Research use only, not for human use.

zapnometinib is a MEK inhibitor.

zapnometinib is a MEK inhibitor.(In Vitro):Zapnometinib inhibits MEK, with IC50s of 30.96 nM, 357 nM, and 15 nM in cell free kinase assay, A549, MDCK cells and human PBMCs.Zapnometinib reduces the viral titers of the IV H1N1pdm09, H3N2.(In Vivo):Zapnometinib exhibits AUC values of 860.02 and 1953.68 μg h/mL in mice by i.v. or oral route, respectively.Zapnometinib reduces the lung virus titers and enhances survival of mice after lethal H1N1pdm09 infection.

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

Animal Model:Female C57BL/6 mice (8 weeks; 21-24 g) were infected with H1N1pdm09 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.

2-(2-chloro-4-iodoanilino)-3,4-difluorobenzoic acid | PD0184264 | ATR-002

Microbiology/Virology

Influenza Virus

Human Endogenous Metabolite

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303175-44-2

409.55

C13H7ClF2INO2

>98% (HPLC)

In Vitro:?DMSO : 62.5 mg/mL (152.61 mM)

OC(c(c(Nc(ccc(I)c1)c1Cl)c1F)ccc1F)=O

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(-20℃)

With Ice Pack

≥ 2 years