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eFT508

Chemical Structure : eFT508

CAS No.: 1849590-01-7

eFT508 (eFT 508;Tomivosertib)

Catalog No.: PC-42035Not For Human Use, Lab Use Only.

eFT508 (Tomivosertib) is a potent, highly selective, reversible, ATP-competitive, and orally bioavailable MNK1 and MNK2 inhibitor with IC50 of 1-2 nM in enzyme assays.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

eFT508 (Tomivosertib) is a potent, highly selective, reversible, ATP-competitive, and orally bioavailable MNK1 and MNK2 inhibitor with IC50 of 1-2 nM in enzyme assays.
eFT508 (Tomivosertib) dose-dependently reduces eIF4E phosphorylation at Serine 209 in tumor cell lines with IC50 of 2-16 nM.
eFT508 (Tomivosertib) shows anti-proliferative activity against multiple DLBCL cell lines, decreases the production of pro-inflammatory cytokines including TNFα, IL-6, IL-10 and CXCL10.
eFT508 (Tomivosertib) demonstrates significant anti-tumor activity in human lymphoma xenograft models which harbor activating MyD88 mutations.

Physicochemical Properties

M.Wt 340.3797
Formula C17H20N6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 6 mg/mL (Need ultrasonic)

Chemical Name/SMILES

Spiro[cyclohexane-1,3'(2'H)-imidazo[1,5-a]pyridine]-1',5'-dione, 6'-[(6-amino-4-pyrimidinyl)amino]-8'-methyl-

References

1. Kevin R. Webster, et al. Blood 2015 126:1554;

2. Dreas A, et al. Curr Med Chem. 2017;24(28):3025-3053.

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