| Identification | Back Directory | [Name]
6'-((6-aminopyrimidin-4-yl)amino)-8'-methyl-1'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridine]-1',5'(2'H)-dione hydrochloride | [CAS]
1849590-02-8 | [Synonyms]
EFT-508.HCL
Tomivosertib HCl
tomivosertib hydrochloride
6'-((6-aminopyrimidin-4-yl)amino)-8'-methyl-1'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridine]-1',5'(2'H)-dione hydrochloride
6'-((6-aminopyrimidin-4-yl)amino)-8'-methyl-1'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridine]-1',5'(2'H)-dione hydrochloride | [Molecular Formula]
C17H21ClN6O2 | [MOL File]
1849590-02-8.mol | [Molecular Weight]
376.85 |
| Hazard Information | Back Directory | [Uses]
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]. | [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. DOI:10.1038/s41591-018-0321-2 |
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