Zapnometinib (Synonyms: PD0184264; ATR-002) |
| Catalog No.GC63264 |
CI-1040의 활성 대사체인 Zapnometinib(PD0184264)는 MEK 억제제로 IC50이 5.7nM입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 303175-44-2
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
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.
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *