Chemical Name: 6-[(6-Aminopyrimidin-4-yl)amino]-8-methylspiro[2H-imidazo[1,5-a]pyridine-3,1-cyclohexane]-1,5-dione. Alternate Names: Tomivosertib
Potent MNK1/2 inhibitor
Molecular Weight:
340.39
Purity:
98% by HPLC NMR (Conforms)
Form:
Pale yellow solid
CAS Number:
[1849590-01-7]
Formula:
C17H20N6O2
Application Notes:
eFT508 is a potent (IC50s = 2.4 nM MNK1, 1.0 nM MNK2) and highly selective inhibitor of the mitogen-activated protein kinase interacting kinases 1 and 2 (MNK1/2), key regulators of mRNA translation protein eukaryotic initiation factor eIF4E.1 It potently inhibits phosphorylation of eIF4E in multiple solid and hematological tumor lines leading to blockade of pro-inflammatory and pro-tumorigenic cytokine production. eFT508 reversed the aggressive and metastatic characteristics of mouse liver cancer via inhibition of PD-L1 upregulation.2 Displays inhibitory effects in various cancers models including acute myeloid leukemia3, gastric4, and breast5. eFT-508 has also shown efficacy in treating neuropathic pain via the MNK-eIF4E pathway.6,7,8
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