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Zotatifin (eFT 226;eFT226) Catalog No. H5735

Zotatifin

CAS No.: 2098191-53-6

Zotatifin(eFT 226;eFT226)

Catalog No.: H5735

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

Biological Activity

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; 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; demonstrates potent inhibition of reporter constructs containing a polypurine motif in the 5'-UTR with IC50 of 2 nM, shows potent anti-proliferative activity (EC50) 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; shows in vivo activity across hematological tumor models. Zotatifin shows robust antiviral effects, it effectively reduces viral infectivity by inhibiting SARS-CoV-2 NP protein biogenesis (IC90=37 nM). Zotatifin induces cell apoptosis.

References

1. Gordon DE, et al.Nature. 2020 Apr 30.

Clinical Information

Solid Tumors
Phase 2 Clinical

Physicochemical Properties

M.Wt 487.55
Formula C28H29N3O5
CAS No. 2098191-53-6
Storage
Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 3 Month
Shipping
Chemical Name/SMILES N#CC1=CC=C([C@@]2(O3)[C@@](C4=C3C=C(OC)N=C4OC)(O)[C@H](O)[C@H](CN(C)C)[C@H]2C5=CC=CC=C5)C=C1

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Eukaryotic Initiation Factor (eIF) Solid Tumors
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