Zapnometinib (Synonyms: PD0184264; ATR-002)
目录号: PL07049 纯度: ≥99%
CAS No. :303175-44-2
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中文名称
Zapnometinib
中文别名
3,4-二氟-2-(2-氯-4-碘苯基氨基)-苯甲酸;7,9-二甲基鸟嘌呤
英文名称
Zapnometinib
英文别名
2-(2-Chloro-4-iodophenylamino)-3,4-difluorobenzoic Acid;2-(2-chloro-4-iodoanilino)-3,4-difluorobenzoic acid;Benzoic acid, 2-[(2-chloro-4-iodophenyl)amino]-3,4-difluoro-;2-(2-chloro-4-iodo-phenylamino)-3,4-difluorobenzoic acid;2-(2-chloro-4-iodo-phenylamino)-3,4-difluoro-benzoic acid;2-[(2-Chloro-4-iodophenyl)amino]-3,4-difluoro-benzoic Acid;AG-E-99770;CHEMBL481949;CTK1C0471;FT-0664738;KB-220861;SureCN1488782;Zapnometinib
Cas No.
303175-44-2
分子式
C13H7NO2F2Cli
分子量
409.55
包装储存
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
产品详情
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。
生物活性
Zapnometinib (PD0184264), an active metabolite of CI-1040, is a MEK inhibitor, with an IC 50 of 5.7 nM. Zapnometinib exhibits antiviral activity against influenza virus and antibacterial activities.
性状
Solid
IC50 & Target[1][2]
MEK 5.7 nM (IC50)
体外研究(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.
Zapnometinib (100 μM; 4 h) inhibits the Ionomycin (PMA/I)-induced phosphorylation of ERK1/2 in human PBMCs.
Zapnometinib (1-100 μM) reduces the viral titers of the IV H1N1pdm09, H3N2. has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis
体内研究(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.
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
ClinicalTrial
参考文献
[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.
溶解度数据
In Vitro: DMSO : 62.5 mg/mL (152.61 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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