Tomivosertib (Synonyms: eFT508)

Name: Tomivosertib
Brand: MedChemExpress
SKU: HY-100022
Rating: 5.0 (11 reviews)

Cat. No.: HY-100022 Purity: 99.92%: FAQs
Data Sheet SDS COA Handling Instructions

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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. Tomivosertib (eFT508) also dramatically downregulates PD-L1 protein abundance.

For research use only. We do not sell to patients.

Tomivosertib Chemical Structure

CAS No. : 1849590-01-7

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 165	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 165	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 230	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 700	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1050	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Tomivosertib:

Tomivosertib hydrochloride Get quote

10 Publications Citing Use of MCE Tomivosertib

: Tomivosertib purchased from MedChemExpress. 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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Biological Activity
Purity & Documentation
References
Customer Review

Description

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

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	GI₅₀	> 50 μM Compound: eFT508	Antiproliferative activity against human A2780 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A2780 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay	[PMID: 31362920]
HCT-116	GI₅₀	27.93 μM Compound: eFT508	Antiproliferative activity against human HCT116 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay	[PMID: 31362920]
HL-60	GI₅₀	> 50 μM Compound: eFT508	Antiproliferative activity against human HL60 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HL60 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay	[PMID: 31362920]
K562	IC₅₀	13.54 μM Compound: eFT508	Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 30824167]
MOLM-13	GI₅₀	33.04 μM Compound: eFT508	Antiproliferative activity against human MOLM13 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MOLM13 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay	[PMID: 31362920]
MV4-11	IC₅₀	14.49 μM Compound: eFT508	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 30824167]
MV4-11	GI₅₀	9.26 μM Compound: eFT508	Antiproliferative activity against human MV4-11 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay	[PMID: 31362920]
PC-3	GI₅₀	> 50 μM Compound: eFT508	Antiproliferative activity against human PC3 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human PC3 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay	[PMID: 31362920]
SK-OV-3	GI₅₀	> 50 μM Compound: eFT508	Antiproliferative activity against human SKOV3 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human SKOV3 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay	[PMID: 31362920]
TMD8	IC₅₀	2.53 μM Compound: eFT508	Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 30824167]

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].

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

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].

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

Clinical Trial

Molecular Weight

340.38

Formula

C₁₇H₂₀N₆O₂

CAS No.

1849590-01-7

Appearance

Solid

Color

Off-white to yellow

SMILES

O=C(C1=C(C)C=C(NC2=NC=NC(N)=C2)C(N13)=O)NC43CCCCC4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 4.35 mg/mL (12.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 0.44 mg/mL (1.29 mM); Clear solution

This protocol yields a clear solution of ≥ 0.44 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (4.4 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.43 mg/mL (1.26 mM); Clear solution

This protocol yields a clear solution of ≥ 0.43 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (4.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: 0.4 mg/mL (1.18 mM); Suspended solution; Need ultrasonic
Protocol 4

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: 0.4 mg/mL (1.18 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.92%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (251 KB) LCMS (111 KB)

Handling Instructions (2659 KB)

References

[1]. Kevin R. Webster, et al. eFT508, a Potent and Selective Mitogen-Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 Inhibitor, Is Efficacious in Preclinical Models of Diffuse Large B-Cell Lymphoma (DLBCL). Blood 2015 126:1554.

[2]. Xu Y, et al. Translation control of the immune checkpoint in cancer and its therapeutic targeting. Nat Med. 2019 Feb;25(2):301-311. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.9379 mL	14.6895 mL	29.3789 mL	73.4473 mL
	5 mM	0.5876 mL	2.9379 mL	5.8758 mL	14.6895 mL
	10 mM	0.2938 mL	1.4689 mL	2.9379 mL	7.3447 mL

Tomivosertib Related Classifications

Help & FAQs

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:

Tomivosertib1849590-01-7eFT508eFT 508eFT-508MNKPD-1/PD-L1Mitogen activated protein kinase interacting kinaseMAP kinase interacting kinaseMAPK interacting kinasePD-1/Programmed death-ligand 1Inhibitorinhibitorinhibit

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Tomivosertib (Synonyms: eFT508)

Customer Review

Other Forms of Tomivosertib:

Tomivosertib Related Antibodies

10 Publications Citing Use of MCE Tomivosertib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All MNK Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Tomivosertib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Tomivosertib Related Classifications

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