Tomivosertib (eFT-508) - Moligand™, ≥97% , Inhibitor of CDC like kinase 4;Inhibitor of MAPK interacting serine/threonine kinase 1;Inhibitor of MAPK interacting serine/threonine kinase 2;Inhibitor of serine/threonine kinase 17a, CAS No.1849590-01-7, Inhibitor of CDC like kinase 4;Inhibitor of MAPK interacting serine/threonine kinase 1;Inhibitor of MAPK interacting serine/threonine kinase 2;Inhibitor of serine/threonine kinase 17a
Tomivosertib (eFT-508) - Moligand™, ≥97% , Inhibitor of CDC like kinase 4;Inhibitor of MAPK interacting serine/threonine kinase 1;Inhibitor of MAPK interacting serine/threonine kinase 2;Inhibitor of serine/threonine kinase 17a, CAS No.1849590-01-7, Inhibitor of CDC like kinase 4;Inhibitor of MAPK interacting serine/threonine kinase 1;Inhibitor of MAPK interacting serine/threonine kinase 2;Inhibitor of serine/threonine kinase 17a
GRADE & PURITYMoligand™?Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools.≥97%
Moligand™, ≥97% Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Storage & shipping
Store at -20°C Ships Ice chest + Ice pads Check lot-specific COA for exact specifications.
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Quality documents
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
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Literature proof
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Overview
Information
Tomivosertib (eFT-508) 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.
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.
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.
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 dramati
Storage
Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of CDC like kinase 4;Inhibitor of MAPK interacting serine/threonine kinase 1;Inhibitor of MAPK interacting serine/threonine kinase 2;Inhibitor of serine/threonine kinase 17a
This compound belongs to the class of organic compounds known as 2-heteroaryl carboxamides. These are compounds containing a heteroaromatic ring that carries a carboxamide group.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
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Application Protocols
No vendor-validated application protocols are provided for this item.
Item-specific
Tested applications, recommended working concentrations, and positive controls: Not specified for this item; refer to CoA/Spec Sheet.
General guidance (use your lab’s SOPs; not product specs)
Stock solutions: Prepare in anhydrous DMSO; sterile-filter if required by your workflow and if solubility permits.
Dosing: Establish a concentration range empirically using vehicle-matched controls; document final DMSO percentage in all treatments.
Readouts: For MNK pathway studies, confirm pharmacodynamics by monitoring phospho-eIF4E (Ser209) reduction via Western blot or phospho-specific assays.
Replicates and controls: Include temporal controls to capture on-target kinetics and recovery after washout.
Always adapt to your assay platform and institutional SOPs; the above is informational and not a substitute for validated protocols.
Biological pathway: Tomivosertib is widely cited as a potent, selective inhibitor of MNK1 and MNK2, kinases that phosphorylate eIF4E at Ser209, a key regulatory node in cap-dependent translation initiation.
Functional consequences: Inhibition of MNK1/2 generally reduces eIF4E phosphorylation, modulating translation of mRNAs involved in stress responses, cell growth, and survival. This makes Tomivosertib a valuable tool for dissecting translational control and its coupling to upstream MAPK signaling (ERK/p38).
Research uses: Employed to probe mechanisms of adaptive resistance, stress granule dynamics, and the selective translation of mRNAs with structured 5′ UTRs. It is also used for pathway deconvolution alongside mTOR/PI3K inhibitors and ribosome profiling studies.
Selectivity considerations: Reports describe high selectivity for MNK1/2 versus broader kinomes, enabling cleaner interpretation of translational changes relative to less selective inhibitors. Nonetheless, orthogonal validation (e.g., genetic knockdown) is recommended to exclude off-target effects in specific models.
Item-specific notes
This listing provides no biological performance specifications. For exact potency/selectivity metrics, consult primary literature and your in-house validation data for the lot in hand.
For research use only; not for diagnostic or therapeutic use.
Buffer Applications
This product is not a buffering agent and is not used to set or maintain pH.
Guidance
Prepare Tomivosertib in an appropriate organic cosolvent (commonly DMSO), then dilute into your chosen biological buffer or culture medium while maintaining a low final cosolvent fraction.
Common biological buffers (PBS, HBSS, HEPES-buffered media) serve as vehicles for delivery but are not altered by the compound to provide buffering capacity.
Not specified for this item
Any pKa values, buffer recipes, or compatibility tables are not provided for this listing; refer to assay-specific literature and conduct pilot tests to confirm solubility and stability under your conditions.
Green Alternatives
Green chemistry comparisons are not directly applicable because Tomivosertib is a specialized bioactive probe, not a solvent or common synthetic auxiliary.
Context
Selection of a chemical probe is driven by biological target specificity and assay performance, not by roles that typically have greener substitutes (e.g., replacing THF with 2-MeTHF).
Practical “green” considerations for handling (general)
Minimize scale: Use micro- to milligram quantities appropriate for screening to reduce waste.
Concentrated stocks: Maintain high-concentration DMSO stocks to limit solvent use and shipping mass.
Waste management: Segregate halogen-free organic waste; neutralize and dispose according to institutional and regulatory requirements.
Data-rich experiments: Employ high-content or multiplexed assays to extract maximal information per unit of compound consumed.
Alternative probes (general comment)
If your objective is to interrogate the MNK–eIF4E pathway with different chemical matter, consider orthogonal MNK1/2 inhibitors or genetic perturbation (e.g., siRNA/CRISPR). Choice should be based on selectivity profile and assay context rather than environmental attributes.
Note: There are no greener “equivalents” in the usual sense for a selective kinase inhibitor; performance and selectivity dominate selection criteria.
Pharmaceutical Uses
Scope of this listing
For research use only. No clinical, diagnostic, or therapeutic use is stated or implied.
Literature/general formulation context (not product specs or claims)
As a reference small-molecule inhibitor, Tomivosertib may be used in preclinical workflows for ADME profiling, permeability/efflux assessments (e.g., Caco-2/MDCK), microsomal stability, and protein binding studies to benchmark translational inhibitor chemotypes.
In discovery settings, it can serve as a positive control to validate MNK pathway assays, phospho-eIF4E readouts, and target engagement methods (e.g., CETSA, NanoBRET), thereby supporting medicinal chemistry optimization without itself being the subject of formulation.
Practical considerations
Stock solution practice: Maintain DMSO stocks at −20°C, aliquoted to reduce freeze–thaw.
Excipient selection for in vivo research is outside the scope of this listing; any such work must follow institutional approvals and is not covered by this product’s intended use.
Not specified for this item
Any pharmacopeial status, excipient compatibility, or dosage-form information: Not specified; refer to CoA/Spec Sheet and relevant regulations.
Physical Properties
Item-specific (Product Data)
Appearance: Not specified for this item; refer to CoA/Spec Sheet.
Molecular weight: Not specified for this item; refer to CoA/Spec Sheet.
Molecular formula: Not specified for this item; refer to CoA/Spec Sheet.
Melting point: Not specified for this item; refer to CoA/Spec Sheet.
Boiling point: Not applicable/unknown for a high-melting solid; not specified for this item.
Density: Not specified for this item; refer to CoA/Spec Sheet.
Refractive index: Not applicable for solids.
Solubility: Not specified for this item; refer to CoA/Spec Sheet.
Literature/general guidance (not product specs)
Handling as a bioactive small molecule typically involves preparing concentrated DMSO stock solutions (e.g., 10–50 mM) due to common hydrophobicity of kinase inhibitors; final working dilutions are made into aqueous buffers or media with ≤0.1–0.5% DMSO cosolvent. Actual solubility for this lot must be verified experimentally.
Partition behavior: Kinase inhibitors often display moderate to high lipophilicity; anticipate adsorption to plastic and consider low-bind labware.
Note: Where exact numeric values are required (e.g., mp, solubility limits), consult the lot-specific CoA/SDS or primary literature. Do not treat the above as item specifications.
Quality & Grades
Item-specific (Product Data)
Grade/Purity designation: Moligand™
Research Use Note: For research use only
What Moligand™ implies (general explanation; not item-specific specs)
Moligand™ denotes inclusion in a curated small-molecule/ligand library intended for discovery, screening, and mechanism-of-action studies. Materials are typically prepared and handled to support reproducible bioassay use, with identity and purity controlled by standard analytical techniques appropriate for small-molecule probes.
Exact analytical methods (e.g., HPLC purity threshold, NMR, MS) and any stabilizers are not specified for this item; refer to the lot-specific CoA/Spec Sheet for definitive details.
Practical notes for this product
As a bioactive kinase inhibitor, Tomivosertib is commonly used as a reference compound or tool molecule in MNK1/2–eIF4E pathway studies. For screening consistency, verify lot identity and purity via the supplied CoA.
If low-adsorption packaging or light protection was used, it will be indicated on the label/CoA. In absence of such notes, store at −20°C and protect from moisture; minimize freeze–thaw cycles by aliquoting.
Not included/unspecified for this listing
Stabilizers, residual solvent limits, water content, metal limits, and UV cutoff: Not specified for this item; refer to CoA/Spec Sheet.
Reaction & Applications
This product is supplied as a bioactive tool compound rather than a synthetic reagent.
Not typically applicable
It is not generally employed as a reagent or catalyst in preparative organic synthesis, and it is not a solvent or auxiliary for standard named reactions.
Relevant research applications (literature/general)
Acts as a chemical probe of the MNK1/2–eIF4E axis, enabling studies of cap-dependent translation, stress-response signaling, and oncogenic translational programs.
Useful as a reference inhibitor in target-validation experiments, orthogonal assay benchmarking, and structure–activity relationship comparisons.
Can serve as a control in phospho-eIF4E (Ser209) readouts (e.g., immunoblotting, phospho-ELISA) when establishing MNK pathway assay windows.
Practical suggestions (general)
Prepare a fresh DMSO stock or use aliquoted frozen stocks to minimize potency drift from adsorption or multiple freeze–thaw cycles.
Include vehicle controls matched for DMSO content; titrate across a relevant concentration range to define IC50/EC50 in your system.
For synthetic transformations or catalyst applications, this product is not recommended; consult our catalog for reagents specifically designed for chemical synthesis.
Reaction Conditions
Not applicable in the conventional synthetic sense. Tomivosertib is not used to catalyze or undergo planned synthetic reactions as part of routine laboratory transformations.
Relevant handling conditions (general for bioassays; not product specs)
Stock preparation: Dissolve in dry DMSO under ambient conditions; vortex and, if necessary, briefly sonicate to ensure complete dissolution.
Storage during use: Keep thawed working stocks on ice, protected from light if photosensitivity is suspected; return to −20°C promptly.
Assay addition: Deliver small volumes of concentrated stock to achieve target concentrations while keeping DMSO low; include matched vehicle controls.
For actual chemical reaction parameters (solvents, catalysts, temperatures), this product is not intended or recommended.
Safety & Handling
Item-specific (Product Data)
GHS Classification: Not specified for this item; refer to SDS.
Signal word: Not specified for this item; refer to SDS.
Hazard statements (H-Statements): Not specified for this item; refer to SDS.
Pictograms: Not specified for this item; refer to SDS.
Storage conditions: Store at −20°C.
Shipping: Ice chest + ice pads.
General laboratory precautions (literature/general; defer to SDS)
PPE: Use laboratory coat, safety glasses, and suitable chemical-resistant gloves. Work in a certified chemical fume hood when handling powders/solutions.
Avoid inhalation of dust or aerosols; prevent contact with skin and eyes. Wash thoroughly after handling.
Incompatibilities: Avoid strong oxidizing agents and strong acids/bases until compatibility is known. Use dry, clean tools to minimize contamination and moisture exposure.
First aid (overview): If inhaled—move to fresh air; skin/eye contact—rinse with water for at least 15 minutes; ingestion—rinse mouth. Seek medical attention per SDS guidance.
Waste: Collect as organic hazardous waste; do not discharge to drains.
Note: No medical or clinical use. For research use only. The SDS is the authoritative source for hazard classification and response procedures.
Solvent Selection
Tomivosertib is a bioactive small molecule rather than a bulk solvent. Solvent selection here refers to dissolving and dispensing the compound for assays.
Item-specific
No solubility data are provided for this item; refer to CoA/Spec Sheet.
Literature/general guidance for similar kinase inhibitors (not product specs)
Primary solvent: DMSO is typically preferred for preparing concentrated stock solutions due to broad solubilizing power for heteroaromatic inhibitors.
Aqueous compatibility: Working solutions are usually prepared by diluting the DMSO stock into buffer or culture media; maintain DMSO below commonly tolerated levels (e.g., ≤0.1–0.5% v/v) depending on the biological system.
Alternative cosolvents: If needed, small amounts of ethanol or DMF can assist solubilization; confirm compatibility with your assay and materials.
Adsorption minimization: Use low-binding polypropylene or glass vials and pre-wet pipette tips with DMSO to improve delivery accuracy at low micromolar concentrations.
Comparison (general)
DMSO: Highest likelihood of complete dissolution; excellent stability for freezer stocks.
Ethanol: Useful for less lipophilic molecules; higher volatility may complicate dosing.
Aqueous buffers: Direct dissolution is often limited for hydrophobic inhibitors; typically used only after DMSO pre-dissolution.
Always confirm solubility and compatibility empirically with your specific lot and assay.
Storage & Reconstitution
Item-specific (Product Data)
Storage temperature: Store at −20°C.
Shipping: Ice chest + ice pads.
Reconstitution
Reconstitution solvent, concentration, and stabilizers: Not specified for this item; refer to CoA/Spec Sheet.
General handling guidance (informational; not product specs)
Allow the container to equilibrate to room temperature in a desiccated environment before opening to avoid moisture condensation.
If preparing solutions, anhydrous DMSO is commonly used for small-molecule inhibitors; filter through a low-protein-binding membrane if sterility is required and solubility allows.
Aliquot solutions to minimize freeze–thaw cycles; store aliquots at −20°C or below. Track preparation dates and concentrations on the vial label.
Stability
Shelf-life and solution stability are not specified for this item; consult the CoA/SDS and verify stability under your exact storage and assay conditions prior to critical experiments.
Structure & Identity
Brief overview: Tomivosertib (eFT-508) is a research-grade, small-molecule kinase inhibitor supplied as a Moligand™ library member.
Item-specific (Product Data)
Product name: Tomivosertib (eFT-508)
SKU: T413958
CAS: 1849590-01-7
PubChem CID: 118598754
InChIKey: 124111 (as provided)
Molecular formula: Not specified for this item; refer to CoA/Spec Sheet.
Molecular weight: Not specified for this item; refer to CoA/Spec Sheet.
SMILES: Not specified for this item; refer to CoA/Spec Sheet.
Literature/general identity (for reference; not item-specific specs)
Common description: a potent, selective inhibitor of MNK1/2 (MAP kinase–interacting kinases) used to modulate eIF4E Ser209 phosphorylation in translational control studies.
Structural class: small-molecule heteroaromatic kinase inhibitor scaffold (exact substituents vary by source; consult primary references for definitive structure drawings).
Two-dimensional structure (descriptive)
Not provided in this listing. Consult the product CoA/SDS or authoritative databases (e.g., PubChem CID 118598754) for the exact 2D depiction and stereochemical details.
Synthetic Utility
Tomivosertib is a finished bioactive probe and is not typically used as a reagent, catalyst, or building block in synthetic chemistry.
Not typically applicable
It does not serve as a functional-group transfer reagent, coupling partner, or ligand in common synthetic transformations.
If synthetic derivatization is desired (general comment)
Any semisynthetic modifications (e.g., installation of reporter handles for target engagement assays) should be guided by structure–activity relationship data to avoid disrupting MNK binding. Such work is custom and outside the scope of this catalog entry.
For conventional synthetic needs (cross-couplings, reductions, oxidations, etc.), please consult our catalog of dedicated reagents and catalysts rather than using this bioactive small molecule.
Primary targets: MNK1 (MKNK1) and MNK2 (MKNK2), serine/threonine kinases downstream of ERK and p38 MAPKs.
Mechanistic outcome: Inhibition of MNK1/2 activity leading to decreased phosphorylation of eIF4E at Ser209, affecting cap-dependent translation of select mRNAs.
Use as a probe: Employed to interrogate the MNK–eIF4E node in translational control, stress signaling, and adaptive resistance models. Frequently used alongside orthogonal inhibitors and genetic perturbations for pathway validation.
Item-specific information
This listing does not include quantitative potency (e.g., IC50/Ki) or kinome selectivity panels. Consult primary literature and perform in-assay titration and target engagement measurements to establish activity in your system.
Note: Target binding and selectivity can vary with cell type, protein expression, and assay conditions; verify with appropriate controls (e.g., phospho-eIF4E immunoblotting, CETSA/NanoBRET).
Frequently Asked Questions
What is the purity of this product?
This product is supplied at ≥97% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.
What is Moligand??
Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.
How should this product be stored?
Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.
How is this product shipped?
This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.
What are the CAS number, molecular formula and molecular weight?
The CAS Number is 1849590-01-7, the molecular formula is C17H20N6O2, and the molecular weight is 340.38 g/mol. InChIKey HKTBYUWLRDZAJK-UHFFFAOYSA-N.
What documentation is provided?
Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.
Need help choosing the grade?
Our grade selection guide covers purity, stabilizer status, and application suitability for all variants in our catalog.
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