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

Tomivosertib (Synonyms: eFT508)

目录号: HY-100022 纯度: 99.92%
产品使用指南

Tomivosertib (eFT508) 是一种有效的,高度选择性的,口服活性的 MNK1MNK2 抑制剂,IC50 值均为 1-2 nM。Tomivosertib (eFT508) 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 (eFT508) 还显著下调 PD-L1 蛋白的丰度。

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Tomivosertib Chemical Structure

Tomivosertib Chemical Structure

CAS No. : 1849590-01-7

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2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1573
In-stock
1 mg ¥750
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5 mg ¥2100
In-stock
10 mg ¥3100
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50 mg ¥7900
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100 mg ¥11250
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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Top Publications Citing Use of Products

    Tomivosertib purchased from MCE. Usage Cited in: Oncogene. 2021 Feb 9.

    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.

    查看 MNK 亚型特异性产品:

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Tomivosertib (eFT508) is a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. Tomivosertib (eFT508) treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50=2-16 nM) in tumor cell lines[1]. Tomivosertib (eFT508) also dramatically downregulates PD-L1 protein abundance[2].

    IC50 & Target[1]

    MNK1

    1-2 nM (IC50)

    MNK2

    1-2 nM (IC50)

    PD-L1

     

    体外研究
    (In Vitro)

    Tomivosertib (eFT508) reduces eIF4E phosphorylation dose-dependently at serine 209 (IC50=2-16 nM) in tumor cell lines. In a panel of appr 50 hematological cancers, Tomivosertib shows anti-proliferative activity against multiple DLBCL cell lines. Sensitivity to Tomivosertib in TMD8, OCI-Ly3 and HBL1 DLBCL cell lines is associated with dose-dependent decreases in production of pro-inflammatory cytokines including TNFα, IL-6, IL-10 and CXCL10. Further evaluation Tomivosertib mechanism of action demonstrates that decreased TNFα production correlates with a 2-fold decrease in TNFα mRNA half-life[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    Tomivosertib (eFT508) shows significant anti-tumor activity in the TMD8 and HBL-1 ABC-DLBCL models, both of which harbor activating MyD88 mutations. Besides, Tomivosertib combines effectively with components of R-CHOP and with novel targeted agents, including PCI-32765 and Venetoclax, in human lymphoma models[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    分子量

    340.38

    Formula

    C17H20N6O2

    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : 4.35 mg/mL (12.78 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.9379 mL 14.6895 mL 29.3789 mL
    5 mM 0.5876 mL 2.9379 mL 5.8758 mL
    10 mM 0.2938 mL 1.4689 mL 2.9379 mL
    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 0.44 mg/mL (1.29 mM); Clear solution

      此方案可获得 ≥ 0.44 mg/mL (1.29 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 4.4 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    • 2.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 0.43 mg/mL (1.26 mM); Clear solution

      此方案可获得 ≥ 0.43 mg/mL (1.26 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 4.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
    • 3.

      请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% saline

      Solubility: 0.4 mg/mL (1.18 mM); Suspended solution; Need ultrasonic

    • 4.

      请依序添加每种溶剂: 5% DMSO    95% (20% SBE-β-CD in saline)

      Solubility: 0.4 mg/mL (1.18 mM); Suspended solution; Need ultrasonic

    *以上所有助溶剂都可在 MCE 网站选购。
    参考文献

    纯度: 99.92%

    • 摩尔计算器

    • 稀释计算器

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
    × = ×
    C1   V1   C2   V2

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    产品名称:
    Tomivosertib
    目录号:
    HY-100022
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