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zapnometinib

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

Print datasheet

Synonyms

CI-1040|ATR 002|ATR002|ATR-002|Bacterial|2-(2-chloro-4-iodoanilino)-3,4-difluorobenzoic acid|3,4-difluoro-2-(2-chloro-4-iodophenylaMino)-benzoic acid|antibacterial|antiviral|InfluenzaVirus|Influenza Virus|influenza|inhibit|PD0184264|PD-0184264|PD 0184264|Inhibitor|MAPKK|MAP2K|MEK|Mitogen-activated protein kinase kinase|zapnometinib|virus

验证数据展示

  • CAS No.: 303175-44-2

    zapnometinib
    CAS#: 303175-44-2

产品信息

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|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 | Shipping with blue ice.
别名 CI-1040|ATR 002|ATR002|ATR-002|Bacterial|2-(2-chloro-4-iodoanilino)-3,4-difluorobenzoic acid|3,4-difluoro-2-(2-chloro-4-iodophenylaMino)-benzoic acid|antibacterial|antiviral|InfluenzaVirus|Influenza Virus|influenza|inhibit|PD0184264|PD-0184264|PD 0184264|Inhibitor|MAPKK|MAP2K|MEK|Mitogen-activated protein kinase kinase|zapnometinib|virus

靶点活性

MEK:5.7 nM

体内活性

Zapnometinib 在小鼠体内，通过静脉(iv)给药展现出860.02 μgh/mL的AUC值，而通过口服给药则为1953.68 μgh/mL[1]。此外，Zapnometinib 能够降低小鼠在致命H1N1pdm09感染后的肺部病毒滴度，并提高存活率[1]。

体外活性

Zapnometinib通过抑制MEK来发挥作用，其在无细胞激酶实验中的IC50为30.96 nM，在A549细胞、MDCK细胞及人类PBMCs中的IC50分别为357 nM和15 nM[1]。此外，Zapnometinib还能降低IV H1N1pdm09、H3N2的病毒滴度[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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