1849590-02-8
Chemical Structure
Tomivosertib hydrochloride
Synonym(s): eFT508 hydrochloride
- CAS No.: 1849590-02-8
- Formula:C17H21ClN6O2
- Molecular Weight:376.84
IUPAC Name: 6'-((6-aminopyrimidin-4-yl)amino)-8'-methyl-2'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridine]-1',5'-dione hydrochloride
InChIKey: WBGPPUUXCGKTSC-UHFFFAOYSA-N
SMILES: O=C(C1=C(C)C=C(NC2=NC=NC(N)=C2)C(N13)=O)NC43CCCCC4.Cl
Biological Activity: 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].
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Tomivosertib hydrochloride | 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. Tomivosertib hydrochloride also dramatically downregulates PD-L1 protein abundance. | |||||||||||||||||||||
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- [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]
Keywords
