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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-MNK-ETC-168
ETC-168

Chemical Structure : ETC-168

CAS No.: 1464150-99-9

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ETC-168 (ETC168)

货号: PC-72233Not For Human Use, Lab Use Only.

ETC-168 (ETC168) is a potent, selective MNK kinase inhibitor with biochemical IC50 of 23 and 43 nM against MNK1 and MNK2, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    ETC-168 (ETC168) is a potent, selective MNK kinase inhibitor with biochemical IC50 of 23 and 43 nM against MNK1 and MNK2, respectively.
    ETC-168 acts as a MNK2-biased, dual-MNK inhibitor in cells.
    ETC-168 induced dose-dependent growth suppression and inhibited 50% of cell viability at 5 uM in LPS141 and MESSA, ETC-168 treatment elicited a consistent increase of cells in G0/G1 phase among LPS141, LP6, and MESSA cells in a dose-dependent manner. ETC-168 decreased cells of S and G2/M phases, while no significant induction of sub-G1 cells.
    Inhibition of MNK1/2 by ETC-168 elevated the expression of MNK1/2 at both transcript and protein levels in soft tissue sarcoma (STS) cells.
    ETC-168 effectively suppressed both p-4E and cell viability in MESSA cells, but not CGP57380 and eFT508.
    ETC-168 suppresseed phosphorylation of ribosomal protein S6 (RPS6) in sensitive STS cell, decreased expression of E2F1, FOXM1, and WEE1.
    Inhibition of MCL1 via S63845 synergizes with ETC-168 against STS cells.

    物理化学性质&存储条件

    分子量 409.449
    分子式 C24H19N5O2
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    4-(6-(4-(morpholine-4-carbonyl)phenyl)imidazo[1,2-b]pyridazin-3-yl)benzonitrile

    参考文献

    1. Haiyan Yang, et al. J Med Chem. 2018 May 24;61(10):4348-4369.

    2. Xin-Yu Ke, et al. Oncogene. 2021 Mar;40(10):1851-1867.

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