Tomivosertib (eFT-508) - 97%, high purity , CAS No.1849590-01-7, Inhibitor of CDC like kinase 4;Inhibitor of MAPK interacting serine/threonine kinase 1;Inhibitor of MAPK interacting serine/threonine kinase 2;Inhibitor of serine/threonine kinase 17a

Item Number

T413958

• Synonyms: Tomivosertib|eFT508|1849590-01-7|EFT-508|Tomivosertib [INN]|Tomivosertib [USAN]|EFT 508|U2H19X4WBV|6-[(6-aminopyrimidin-4-yl)amino]-8-methylspiro[2H-imidazo[1,5-a]pyridine-3,1'-cyclohexane]-1,5-dione|CHEMBL4073443|6'-((6-aminopyrimidin-4-yl)amino)-8'-meth
• Specifications & Purity: Moligand™, ≥97%
• Biochemical and Physiological Mechanisms: Tomivosertib (eFT-508) is a potent and selective MNK1/2 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 eIF4E phosphorylation and dramati
• Storage Temp: Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: Inhibitor of CDC like kinase 4;Inhibitor of MAPK interacting serine/threonine kinase 1;Inhibitor of MAPK interacting serine/threonine kinase 2;Inhibitor of serine/threonine kinase 17a

Product Description

Information

Tomivosertib (eFT-508) Tomivosertib (eFT-508) is a potent and selective MNK1/2 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 eIF4E phosphorylation and dramatically downregulates PD-L1 protein abundance.

Targets

MNK2 (Cell-free assay); MNK1 (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.

In vivo

eFT508 is well-tolerated and shows efficacy against MyD88-mutant DLBCL models in vivo. Significant anti-tumor activity of eFT508 is observed in the TMD8 and HBL-1 ABC-DLBCL models(subcutaneous human lymphoma xenograft models), both of which harbor activating MyD88 mutations.

Cell Research(from reference)

Cell lines：TMD8 cells 

Concentrations：0.01, 0.1, 1, 3, 10 μM 

Incubation Time：24 h