[CAS NO. 1849590-01-7] Tomivosertib (eFT-508)

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [1849590-01-7]

Catalog

SLK-S8275

Brand

Selleck

CAS

1849590-01-7

DESCRIPTION [1849590-01-7]

Overview

MDL	MFCD30489732
Molecular Weight	340.38
Molecular Formula	C17H20N6O2
SMILES	O=C(C1=C(C)C=C(NC2=NC=NC(N)=C2)C(N13)=O)NC43CCCCC4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume 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
50 mM	-	-	-

Description

Tomivosertib (eFT-508) is a potent and selective 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 phosphorylation and dramatically downregulates protein abundance.

Targets

MNK2 ^[1] (Cell-free assay)	MNK1 ^[1] (Cell-free assay)
1 nM	2.4 nM

In vitro

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.

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). Abstract#1554.