Tomivosertib (Synonyms: eFT508)

Name: Tomivosertib
Brand: MedChemExpress
SKU: HY-100022
Rating: 5.0 (13 reviews)

Cat. No.: HY-100022 Purity: 99.75%: Data Sheet
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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.

CAS No. : 1849590-01-7

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of Tomivosertib:

Tomivosertib hydrochloride Get quote

13 Publications Citing Use of MCE Tomivosertib

Cell Imaging/Staining

Others

Bio/Physico-chemical Assay

: Tomivosertib purchased from MedChemExpress. Usage Cited in: Brain. 2024 Jul 24:awae178. [Abstract]; MNK inhibition with eFT508 (Tomivosertib: 25 nM) rapidly decreases phosphorylated eIF4E in human dorsal root ganglion neurons. Representative enlarged images of p-eIF4E immunostaining (red) and neuronal marker, peripherin (blue).

: Tomivosertib purchased from MedChemExpress. Usage Cited in: Brain. 2024 Jul 24:awae178. [Abstract]; Treatment with eFT508 (Tomivosertib: 25 nM) reverses spontaneous activity in human dorsal root ganglion neurons associated with painful dermatomes.

: Tomivosertib purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2022 Sep;18(9):942-953. [Abstract]; Immunoblot analysis was performed on PANC-1 cell lysates to detect the expression of phosphorylated eIF4E (Ser 209; p-eIF4E), total eIF4E, and actin. These cells were treated with DMSO, CID661578, cercariaein, CGP57380, or eFT508 (Tomivosertib: 40 μM) for 6 hours.

: Tomivosertib purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2022 Sep;18(9):942-953. [Abstract]; Six-day-old zebrafish larvae underwent β-cell ablation and were treated with DMSO, CID661578, eFT508, or a combination of CID661578 and eFT508 (Tomivosertib: 10 μM) for 48 hours. The number of β-cells was then quantitatively analyzed.

: Tomivosertib purchased from MedChemExpress. Usage Cited in: Oncogene. 2021 Mar;40(10):1851-1867. [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]
A549	IC₅₀	> 50 μM Compound: eFT508; 1	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 38564512]
DOHH-2	IC₅₀	6.3 μM Compound: eFT508; 1	Antiproliferative activity against human DOHH-2 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human DOHH-2 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 38564512]
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]
HT-29	IC₅₀	> 50 μM Compound: eFT508; 1	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 38564512]
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]
LN-18	IC₅₀	6.27 μM Compound: eFT508; 1	Antiproliferative activity against human LN-18 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human LN-18 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 38564512]
MDA-MB-231	IC₅₀	45 μM Compound: eFT508; 1	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 38564512]
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	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]
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]
PANC-1	IC₅₀	> 50 μM Compound: eFT508; 1	Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 38564512]
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]
PC-3	IC₅₀	29.4 μM Compound: eFT508; 1	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 38564512]
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]
TMD8	IC₅₀	> 50 μM Compound: eFT508; 1	Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 38564512]

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 : 8 mg/mL (23.50 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
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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

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.75%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (251 KB) HNMR (183 KB) RP-HPLC (222 KB) MS (69 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
	15 mM	0.1959 mL	0.9793 mL	1.9586 mL	4.8965 mL
	20 mM	0.1469 mL	0.7345 mL	1.4689 mL	3.6724 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

13 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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