Tomivosertib (eFT-508)

This product is for research use only, not for human use. We do not sell to patients.

For small sizes, please check our retail website as below: www.invivochem.com

Size	Price	Stock
100mg	$1150	In Stock
250mg	$1850	In Stock
500mg	$2775	In Stock

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Cat #: V2662 CAS #: 1849590-01-7 Purity ≥ 98%

Description: Tomivosertib (also known as eFT508) is a potent, highly selective, reversible, ATP-competitive and orally bioavailable inhibitor of MNK1 and MNK2 (Mitogen-Activated Protein Kinase Interacting Kinase) with IC50 values of 1-2 nM against both isoforms in enzyme assays.

References: 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.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	340.38
Molecular Formula	C17H20N6O2
CAS No.	1849590-01-7
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 13 mg/mL (38.2 mM)r
	Water: <1 mg/mLr
	Ethanol: <1 mg/mL
SMILES Code	NC1=NC=NC(NC2=CC(C)=C3N(C4(CCCCC4)NC3=O)C2=O)=C1
Synonyms	Tomivosertib; eFT-508; eFT 508; eFT508

Protocol	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.
Protocol	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.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	2.9379 mL	14.6895 mL	29.3789 mL	58.7579 mL
5mM	0.5876 mL	2.9379 mL	5.8758 mL	11.7516 mL
10mM	0.2938 mL	1.4689 mL	2.9379 mL	5.8758 mL
20mM	0.1469 mL	0.7345 mL	1.4689 mL	2.9379 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

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: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

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

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

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 add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.