zapnometinib

Zapnometinib (ATR-002) 是 CI-1040 的活性代谢物,是一种 MEK 抑制剂,IC50值为 5.7 nM,有抗流感病毒的抗病毒和抗菌活性。

CAS号

303175-44-2

分子式

C13H7ClF2INO2

主要靶点

Antibacterial|Influenza Virus|MEK

仅限科研使用

Cat No : CM05047

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Synonyms

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



产品信息

Zapnometinib (ATR-002) is a MEK inhibitor.

CAS号 303175-44-2
分子式 C13H7ClF2INO2
主要靶点 Antibacterial|Influenza Virus|MEK
主要通路 MAPK信号通路|微生物学
分子量 409.55
纯度 99.66%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 3,4-difluoro-2-(2-chloro-4-iodophenylaMino)-benzoic acid|ATR-002|PD0184264|2-(2-chloro-4-iodoanilino)-3,4-difluorobenzoic acid

靶点活性

MEK:5.7 nM

体内活性

Zapnometinib exhibits AUC values of 860.02 and 1953.68 μg?h/mL in mice by i.v. or oral route, respectively[1].Zapnometinib reduces the lung virus titers and enhances survival of mice after lethal H1N1pdm09 infection[1].

体外活性

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[1].Zapnometinib reduces the viral titers of the IV H1N1pdm09, H3N2[1].

溶解度

DMSO:60 mg/mL (146.50 mM)

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

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