eFT508 MedChemExpress (MCE)

Product Name	EFT-508
Synonyms	EFT-508 CS-2450 eFT-508 eFT508 -MNK Tomivosertib eFT-508 (eFT508) Tomivosertib eFT508 Synonyms EFT-508 CS-2450 eFT-508 eFT508 -MNK Tomivosertib eFT-508 (eFT508) Tomivosertib eFT508 6'-[(6-Amino-4-pyrimidinyl)amino]-8'-methylspiro[cyclohexane-1,3'(2'H)-imidazo[1,5-a]pyridine]-1',5'-dione 6'-((6-aminopyrimidin-4-yl)amino)-8'-methyl-1'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridine]-1',5'(2'H)-dione
CAS	1849590-01-7
EINECS
Chemical Formula	C17H20N6O2
Molecular Weight	340.3797
inchi
Package	10 mM * 1 mL;1 mg;5 mg;10 mg;25 mg
Price	Email to quote
Descriptions	Tomivosertib Tomivosertib MedChemExpress (MCE) HY-100022 1849590-01-7 eFT508 99.92% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions Tomivosertib Tomivosertib MedChemExpress (MCE) HY-100022 1849590-01-7 eFT508 99.92% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. 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. 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]. 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]. MNK1 1-2 nM (IC50) MNK2 1-2 nM (IC50) PD-L1 \| \| \| \| \| \| \| \| \| \| [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]
Last Update	2025-04-01 14:45:47

MedChemExpress (MCE) also provides

Thalidomide-4-O-C2-NH2

Category: Signaling Pathways
CAS: 2341840-99-9
Last Update: 2025-04-01 14:45:47

PPARα-MO-1

Category: Signaling Pathways
CAS: 810677-36-2
Last Update: 2025-04-01 14:45:47

Netupitant N-oxide

Category: Signaling Pathways
CAS: 910808-11-6
Last Update: 2025-04-01 14:45:47

MK-0812

Category: Signaling Pathways
CAS: 624733-88-6
Last Update: 2025-04-01 14:45:47

TS-011

Category: Signaling Pathways
CAS: 339071-18-0
Last Update: 2025-04-01 14:45:47

SCH 530348 sulfate

Category: Signaling Pathways
CAS: 705260-08-8
Last Update: 2025-04-01 14:45:47

BAG 956

Category: Signaling Pathways
CAS: 853910-02-8
Last Update: 2025-04-01 14:45:47

YM758

Category: Signaling Pathways
CAS: 312752-85-5
Last Update: 2025-04-01 14:45:47


Supplier Name	MedChemExpress (MCE)
Contact	sales
Tel	609-228-6898
Mobile	609-228-6898
QQ
Email	sales@medchemexpress.com; tech@medchemexpress.com
Website	https://www.medchemexpress.com/
Wechat

Request for quotation

Supplier Contact