eFT508 | Potent MNK1/2 inhibitor

CAS:
 1849590-01-7
Catalog Number:
 10-4081

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eFT508 (1849590-01-7) 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

References/Citations:

  1. Reich et al. (2018), Structure-based design of Pyridone-Aminal eFT508 Targeting Dysregulated Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1 and 2 (MNK1/2) Inhibition; J.Med.Chem. 61 3516
  2. Xu et al. (2019), Translation control of the immune checkpoint in cancer and its therapeutic targeting; Nat. Med. 25 301
  3. Suarez et al. (2021), Inhibitory effects of Tomivosertib in acute myeloid leukemia; Oncotarget 12 955
  4. Yang et al. (2022), Inhibition MNL-eIF4E-ß-catenin preferentially sensitizes gastric cancer to chemotherapy; Fundam. Clin. Pharmacol. 36 712
  5. Yang et al. (2022), Treatment with eFT-508 increases chemosensitivity in breast cancer cells by modulating the tumor microenvironment; J. Transl. Med. 20 276
  6. Megat et al. (2019), Nociceptor Translational Profiling Reveals the Ragulator-Rag GTPase Complex as a Critical Generator of Neuropathic Pain; J. Neurosci. 39 393
  7. Shiers et al. (2020), Reversal of peripheral nerve injury-induced neuropathic pain and cognitive dysfunction via genetic and tomivosertib targeting of MNK; Neuropsychopharmacology 45 524
  8. Jeevakumar et al. (2020), IL-6 induced upregulation of T-type Ca2+ currents and sensitization of DRG nociceptors is attenuated by MNK inhibition; J. Neurophysiol. 124 274
CAS:
1849590-01-7
Catalog Number:
10-4081
Activity:
Potent MNK1/2 inhibitor
Chemical Names:
6-[(6-Aminopyrimidin-4-yl)amino]-8-methylspiro[2H-imidazo[1,5-a]pyridine-3,1’-cyclohexane]-1,5-dione
Alternate Name:
Tomivosertib
Molecular Weight:
340.39
Molecular Formula:

C17H20N6O2

Solubility:
Soluble in DMSO (2 mg/mL with warming)
Physical Properties:
Pale yellow solid
Purity:

98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO or water may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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