Home MAPK MNK inhibitor - eIF inhibitor - PD-1/PD-L1 inhibitor Tomivosertib (eFT-508)

Tomivosertib (eFT-508)

Catalog No.S8275

For research use only.

Tomivosertib (eFT-508) is a potent and selective MNK1/2 inhibitor with IC50s of 2.4 nM and 1 nM, respectively. It potentially results in decreased tumor cell proliferation and tumor growth. Tomivosertib (eFT-508) inhibits eIF4E phosphorylation and dramatically downregulates PD-L1 protein abundance.

Tomivosertib (eFT-508) Chemical Structure

CAS No. 1849590-01-7

Selleck's Tomivosertib (eFT-508) has been cited by 7 Publications

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Biological Activity

Description Tomivosertib (eFT-508) is a potent and selective MNK1/2 inhibitor with IC50s of 2.4 nM and 1 nM, respectively. It potentially results in decreased tumor cell proliferation and tumor growth. Tomivosertib (eFT-508) inhibits eIF4E phosphorylation and dramatically downregulates PD-L1 protein abundance.
Targets
MNK2 [1]
(Cell-free assay)		 MNK1 [1]
(Cell-free assay)
1 nM 2.4 nM
In vitro

eFT508 has a half-maximal inhibitory concentration (IC50) of 1-2 nM against both MNK isoforms in enzyme assays and inhibits the kinase through a reversible, ATP-competitive mechanism of action. Treatment of tumor cell lines with eFT508 leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50 = 2-16 nM). In a panel of ~50 hematological cancers, eFT508 shows anti-proliferative activity against multiple DLBCL cell lines. Sensitivity to eFT508 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[1].
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
TMD8 NFPU[ZBHfW6ldHnvckBie3OjeR?= NGPuVFYxNjBzLDCwMlEtKDFuIEOgZY5lKDFyIN88US=> M{TZXlIhcA>? NWW1RoN[eG:2ZX70JIRwe2VvZHXw[Y5l\W62IHnubIljcXSrb36gc4Yh\UmINFWgV4VzOjB7IIDoc5NxcG:{eXzheIlwdg>? NX[3UmpPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NlYxQThpPkK5OVI3ODl6PD;hQi=>
TMD8 MUnQdo9tcW[ncnH0bY9vKGG|c3H5 Ml:zNVIhcA>? MUDJR|UxRTJwNUOg{txO M3S3fFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyOEK0NVY4Lz5|MEiyOFE3PzxxYU6=
MV4-11 M2LPeXBzd2yrZnXyZZRqd25iYYPzZZk> M2\CSlEzKGh? MmPxTWM2OD1zND60PUDPxE1? NFfEe4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEiyOFE3Pyd-M{C4NlQyPjd:L3G+
K562  M4nWdXBzd2yrZnXyZZRqd25iYYPzZZk> MlrKNVIhcA>? Mnf1TWM2OD1zMz61OEDPxE1? MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODh{NEG2O{c,OzB6MkSxOlc9N2F-
Vero E6 NHLvbJpCdnSrdnnyZYwh[XO|YYm= MmPGOFghcA>? MomyTWM2OCCob4KgZY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgV2FTWy2Fb2[tNkBqdiC2aHWgWoVzdyCHNjDj[YxtKGyrbnWgZZQhPDhiaDDifUBqdW23bn;mcJVwemW|Y3XuZ4Uu[mG|ZXSgZZN{[XliKHTleIVkfGmwZzD0bIUhfmm{YXygUnAheHKxdHXpckBqdiC2aHWgcpVkdGW3czDv[kB1cGViVnXyc{BGPiClZXzsd{kvNCCLQ{WwJF0hOC5|NE[3OEDPxE1w NGTje3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MkO1N|g2QSd-M{KzOVM5PTl:L3G+
Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot p-eIF4E 30459229
Growth inhibition assay Cell viability 30832411
In vivo

eFT508 is well-tolerated and shows efficacy against MyD88-mutant DLBCL models in vivo. Significant anti-tumor activity of eFT508 is observed in the TMD8 and HBL-1 ABC-DLBCL models(subcutaneous human lymphoma xenograft models), both of which harbor activating MyD88 mutations[1].

Protocol (from reference)

Cell Research:

[1]
  • Cell lines: TMD8 cells
  • Concentrations: 0.01, 0.1, 1, 3, 10 μM
  • Incubation Time: 24 h
  • Method:

    TMD8 cells are treated with the indicated concentrations of eFT508 for 24 h. Cell lysates are subjected to m7-GTP Sepharose pull-down and bound proteins are analyzed by immunoblotting with the indicated antibodies.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 340.38
Formula

C17H20N6O2
CAS No. 1849590-01-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C2C(=O)NC3(N2C(=O)C(=C1)NC4=NC=NC(=C4)N)CCCCC3

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04622007 Recruiting Drug: Tomivosertib|Biological: Pembrolizumab Non-small Cell Lung Cancer Effector Therapeutics|Medpace Inc. June 2 2021 Phase 2
NCT04261218 Recruiting Drug: tomivosertib|Drug: paclitaxel Breast Cancer Translational Research in Oncology|Effector Therapeutics|Stand Up To Cancer August 25 2020 Phase 1
NCT02937675 Terminated Drug: Tomivosertib (eFT-508) Lymphoma Effector Therapeutics February 8 2017 Phase 1|Phase 2
NCT02605083 Terminated Drug: eFT508 Cancer Effector Therapeutics December 3 2015 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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