Tomivosertib hydrochloride (Synonyms: eFT508 hydrochloride)

Cat. No.: HY-100022A: FAQs
Data Sheet Handling Instructions Technical Support

Tomivosertib hydrochlorideis a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC₅₀s of 1-2 nM against both isoforms. Tomivosertib hydrochloride treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC₅₀=2-16 nM) in tumor cell lines. Tomivosertib hydrochloride also dramatically downregulates PD-L1 protein abundance.

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

Tomivosertib hydrochloride Chemical Structure

CAS No. : 1849590-02-8

Size		Stock
MOQ		Minimum order quantity
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote
Other size		Get quote

Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of Tomivosertib hydrochloride:

Tomivosertib

Other Forms of Tomivosertib hydrochloride:

Tomivosertib In-stock

10 Publications Citing Use of MCE Tomivosertib hydrochloride

: Tomivosertib hydrochloride 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.

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

View All MNK Isoform Specific Products:

View All Isoforms

MNK1 MNK2 MNK

Biological Activity
Purity & Documentation
References
Customer Review

Description

Tomivosertib hydrochlorideis a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC₅₀s of 1-2 nM against both isoforms. Tomivosertib hydrochloride treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC₅₀=2-16 nM) in tumor cell lines^[1]. Tomivosertib hydrochloride also dramatically downregulates PD-L1 protein abundance^[2].

IC₅₀ & Target

IC50: 1-2 nM (MNK1), 1-2 nM (MNK2)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	1 nM Compound: eFT-508	Inhibition of MNK2 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis Inhibition of MNK2 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis	[PMID: 30530193]
HEK293	IC₅₀	2 nM Compound: eFT-508	Inhibition of MNK1 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis Inhibition of MNK1 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis	[PMID: 30530193]

Molecular Weight

376.84

Formula

C₁₇H₂₁ClN₆O₂

CAS No.

1849590-02-8

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

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]

Tomivosertib hydrochloride Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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:

Tomivosertib1849590-02-8eFT508eFT 508eFT-508MNKPD-1/PD-L1Mitogen activated protein kinase interacting kinaseMAP kinase interacting kinaseMAPK interacting kinasePD-1/Programmed death-ligand 1Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks