2. MAPK/ERK Pathway Immunology/Inflammation
  3. MNK PD-1/PD-L1
  4. Tomivosertib hydrochloride

Tomivosertib hydrochloride  (Synonyms: eFT508 hydrochloride)

目录号: HY-100022A
产品使用指南 技术支持

Tomivosertib (eFT508 hydrochloride) hydrochloride 是一种有效的，高度选择性的，口服活性的 MNK1 和 MNK2 抑制剂，IC50 值均为 1-2 nM。Tomivosertib hydrochloride 处理可降低肿瘤细胞中 eIF4E 的磷酸化水平 (位点为 Ser209，IC50=2-16 nM)。Tomivosertib hydrochloride 还显著下调 PD-L1 蛋白的丰度。

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Tomivosertib hydrochloride Chemical Structure

Tomivosertib hydrochloride Chemical Structure

CAS No. : 1849590-02-8

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Tomivosertib hydrochloride 的其他形式现货产品:

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Tomivosertib hydrochloride 相关抗体

Top Publications Citing Use of Products

    Tomivosertib hydrochloride purchased from MCE. Usage Cited in: Oncogene. 2021 Feb 9.  [Abstract]

    Protein levels of eIF4E and MCL1 in LPS141 and MESSA cells upon treatment with eFT508 (30 μM, 24 h). The result indicates a inhibition of p-4E at 30 μM.

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    MNK1 MNK2 MNK

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Tomivosertib hydrochlorideis a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. Tomivosertib hydrochloride treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50=2-16 nM) in tumor cell lines[1]. Tomivosertib hydrochloride also dramatically downregulates PD-L1 protein abundance[2].

    IC50 & Target

    IC50: 1-2 nM (MNK1), 1-2 nM (MNK2)[1]
    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HEK293 IC50
    1 nM
    Compound: eFT-508
    Inhibition of MNK2 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis
    Inhibition of MNK2 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis
    		[PMID: 30530193]
    HEK293 IC50
    2 nM
    Compound: eFT-508
    Inhibition of MNK1 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis
    Inhibition of MNK1 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis
    		[PMID: 30530193]
    分子量

    376.84

    Formula

    C17H21ClN6O2
    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献

    Tomivosertib hydrochloride 相关分类

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Tomivosertib1849590-02-8eFT508eFT 508eFT-508MNKPD-1/PD-L1Mitogen activated protein kinase interacting kinaseMAP kinase interacting kinaseMAPK interacting kinasePD-1/Programmed death-ligand 1Inhibitorinhibitorinhibit

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