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Tomivosertib (eFT-508) MNK inhibitor

Name: Tomivosertib (eFT-508)
Brand: Selleck Chemicals
SKU: S8275
Availability: InStock
Rating: 5 (16 reviews)

Cat.No.S8275

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. This compound inhibits eIF4E phosphorylation and dramatically downregulates PD-L1 protein abundance.

Chemical Structure

Molecular Weight: 340.38

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S827501 DMSO]13 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.98%

99.98

Related Targets	Ras ERK p38 MAPK Raf JNK MEK S6 Kinase MAP4K TAK1 Mixed Lineage Kinase ASK MAPKAPK2 KLF TOPK
Related Products	CGP 57380 SEL201

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
TMD8	Function assay	0.01, 0.1, 1, 3 and 10 μM	2 h	potent dose-dependent inhibition of eIF4E Ser209 phosphorylation	29526098
TMD8	Proliferation assay		12 h	IC50=2.53 μM	30824167
MV4-11	Proliferation assay		12 h	IC50=14.49 μM	30824167
K562	Proliferation assay		12 h	IC50=13.54 μM	30824167
Vero E6	Antiviral assay		48 h	IC50 for antiviral activity against SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells)., IC50 = 0.34674 μM.	32353859
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	340.38	Formula	C₁₇H₂₀N₆O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1849590-01-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=C2C(=O)NC3(N2C(=O)C(=C1)NC4=NC=NC(=C4)N)CCCCC3

Solubility

In vitro
Batch:

DMSO : 13 mg/mL ( (38.19 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.650mg/ml (1.91mM)	Taking the 1 mL working solution as an example, add 50 μL of 13 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.312mg/ml (0.92mM)	Taking the 1 mL working solution as an example, add 50 μL of 6.25 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

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

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	MNK2 ^[1] (Cell-free assay) 1 nM MNK1 ^[1] (Cell-free assay) 2.4 nM
In vitro	Tomivosertib (eFT-508) 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 this compound leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50 = 2-16 nM). In a panel of ~50 hematological cancers, this chemical shows anti-proliferative activity against multiple DLBCL cell lines. Sensitivity to this compound 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].
In vivo	Tomivosertib (eFT-508) is well-tolerated and shows efficacy against MyD88-mutant DLBCL models in vivo. Significant anti-tumor activity of this compound is observed in the TMD8 and HBL-1 ABC-DLBCL models(subcutaneous human lymphoma xenograft models), both of which harbor activating MyD88 mutations^[1].
References	http://effector.com/wp-content/uploads/2015/12/eFFECTOR-ASH-2015-poster_final.pdf

Applications

Methods	Biomarkers	Images	PMID
Western blot	p-eIF4E		30459229
Growth inhibition assay	Cell viability		30832411

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05744739	Recruiting	Acute Myeloid Leukemia	Northwestern University\|National Cancer Institute (NCI)\|EFFECTOR Therapeutics Inc.	September 29 2023	Phase 1
NCT04261218	Completed	Breast Cancer	Translational Research in Oncology\|Effector Therapeutics\|Stand Up To Cancer	August 25 2020	Phase 1
NCT02937675	Terminated	Lymphoma	Effector Therapeutics	February 8 2017	Phase 1\|Phase 2
NCT02605083	Terminated	Cancer	Effector Therapeutics	December 3 2015	Phase 1\|Phase 2

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