Zotatifin (eFT226) is a potent, selective, and well-tolerated eIF4A inhibitor. Zotatifin promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs ( IC 50 =2 nM) and interferes with the assembly of the eIF4F initiation complex Zotatifin shows robust antiviral effects, it effectively reduces viral infectivity by inhibiting SARS-CoV-2 NP protein biogenesis ( IC 90 =37 nM) . Zotatifin induces cell apoptosis In Vitro Zotatifin induces the formation of a stable ternary complex [eIF4A-RNA-eFT226]. Zotatifin increases the residence time for eIF4A1 binds to an AGAGAG RNA surface, the K d values are 0.021 μM and 8.0 μM, respectively for eFT226 presence or absence. Zotatifin inhibits in vitro translation as a sequence-dependent manner, the IC 50 values are 1.5 nM, 13.8 nM, 92.5 nM, and 217.5 nM, respectively in an MDA-MB-231 cell line with transiently transfected AGAGAG, GGCGGC, CCGCCG and CAACAA 5’-UTRs-containing sequences. Zotatifin (0.0001 μM-1 μM; 72 hours) inhibits tumor cells growth as a dose-dependent manner. It shows a potent anti-proliferative activity (GI 50 In Vivo Zotatifin (intravenous injection; 1 mg/kg; 14-22 days) decreases tumor volume, inhibits the TMD8 xenograft-bearing, HBL1 xenograft-bearing, Pfeiffer xenograft-bearing, SU-DHL-6 xenograft-bearing, SU-DHL-10 xenograft-bearing and Ramos-bearing animals’tumor growth as percentage of 97%, 87%, 70%, 83%, 37% and 75%, respectively . Zotatifin (intravenous injection; 0.001 mg/kg-1 mg/kg; 15 days) inhibits the growth of B-cell lymphoma xenografts and is well-tolerated against B-cell lymphoma xenograft models in vivo . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: B-cell lymphoma xenograft model Dosage: 0.001 mg/kg; 0.1 mg/kg; 1 mg/kg Administration: Intravenous injection; 15 days Result: Showed efficacy in B-cell lymphoma xenograft models. Form:Solid IC50& Target:eIF4
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Zotatifin
CAS number：2098191-53-6 molecular formula：C28H29N3O5
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| Chinese alias | 佐他替芬 | ||
| English alias | ISOCYANIC ACID, M-ISOPROPENYL-.ALPHA.,.ALPHA.-DIMETHYLBENZYL ESTER | Zotatifin (USAN/INN) | 4-[(2S,3R,4S,5S,6R)-4-[(dimethylamino)methyl]-2,3-dihydroxy-10,12-dimethoxy-5-phenyl-7-oxa-11-azatricyclo[6.4.0.0,dodeca-1(12),8,10-trien-6-yl]benzonitrile | 4-((5 | ||
| CAS number | 2098191-53-6 | molecular formula | C28H29N3O5 |
| molecular weight | 487.55 g/mol | Exact mass | ≥99% |
| PSA | 108.000 Ų | logp | 2.400 |
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