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Chemical Structure : eFT226
CAS No.: 2098191-53-6
Catalog No.: PC-63308Not For Human Use, Lab Use Only.
eFT226 is a novel, potent and selective eIF4A inhibitor with anti-tumor activity in B-cell malignancies, promotes eIF4A binding to specific mRNA sequences and interferes with the assembly of the eIF4F initiation complex.
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Zotatifin (eFT226) is a novel, potent and selective eIF4A inhibitor with anti-tumor activity in B-cell malignancies, promotes eIF4A binding to specific mRNA sequences and interferes with the assembly of the eIF4F initiation complex.
Zotatifin (eFT226) selectively inhibits translation of mRNAs containing longer 5'-UTRs, an increased frequency of uORFs (upstream open reading frame), and polypurine and/or G-quadraplex recognition motifs.
Zotatifin (eFT226) demonstrates potent inhibition of reporter constructs containing a polypurine motif in the 5'-UTR with IC50 of 2 nM.
Zotatifin (eFT226) shows potent anti-proliferative activity (EC50<15 nM) and an induction of apoptosis against a panel of B-cell lymphoma cell lines, dose-dependently decreases the oncogenic drivers c-MYC, CCND1/3, BCL2 or MCL-1.
Zotatifin (eFT226) shows in vivo activity across hematological tumor models.
| M.Wt | 487.55 | |
| Formula | C28H29N3O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
4-[(5aR,6S,7S,8R,8aS)-7-[(Dimethylamino)methyl]-6,7,8,8a-tetrahydro-8,8a-dihydroxy-1,3-dimethoxy-6-phenyl-5aH-cyclopenta[4,5]furo[3,2-c]pyridin-5a-yl]benzonitrile |
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1. Peggy A. Thompson, et al. Preclinical Evaluation of eFT226, a Novel, Potent and Selective eIF4A Inhibitor with Anti-tumor Activity in B-cell Malignancies.
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