Zapnometinib (PD0184264) 是 CI-1040 的活性代谢物，是一种 MEK 抑制剂，IC50 值为 5.7 nM。Zapnometinib 具有抗流感病毒的抗病毒活性和抗菌活性。
货号:ajcx35340
CAS:303175-44-2
分子式:C13H7ClF2INO2
分子量：409.55
溶解度:DMSO : 62.5 mg/mL (152.61 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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].

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].

[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.