纯度:98% by HPLC;NMR (Conforms)
分子式:C17H20N6O2
分子量:340.39
溶剂:DMSO (2 mg/ml with warming)
性状:Pale yellow solid
存储:-20°C
Activity (short version):Potent MNK1/2 inhibitor
Function / Pharmacology: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