Zotatifin

SKU: orb1706438

Description

Zotatifin (eFT226) is a potent and selective inhibitor of eukaryotic initiation factor 4A (eIF4A) with demonstrated antiviral and anticancer properties. It suppresses tumor growth in preclinical models by targeting oncogenic signaling pathways, such as those driven by receptor tyrosine kinases, and induces apoptosis through inhibition of specific oncoprotein synthesis like Sox4. Its activity has been validated in both in vitro and in vivo research studies.

Research Area

Cell Biology, Immunology & Inflammation, Infectious Disease & Virology

Key Properties

• CAS Number: 2098191-53-6
• MW: 487.55
• Purity: 99.61% (May vary between batches)
• Formula: C₂₈H₂₉N₃O₅
• SMILES: O[C@]12[C@]([C@@H]([C@@H](CN(C)C)[C@H]1O)C3=CC=CC=C3)(OC=4C2=C(OC)N=C(OC)C4)C5=CC=C(C#N)C=C5
• Target: SARS-CoV,PERK,Antiviral,Apoptosis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (10.26 mM);DMSO:180 mg/mL (369.19 mM)

Bioactivity

• Target IC50:
  eIF4A:2 nM
• In Vivo:
  Methods: Zotatifin (1 mg/kg, intravenous injection, 14-22 days) was used to treat mice bearing TMD8 xenografts, HBL1 xenografts, Pfeiffer xenografts, SU-DHL-6 xenografts, SU-DHL-10 xenografts, and Ramos xenografts, and the tumor inhibition rate was observed. Results: The tumor growth percentages of various tumor xenograft model mice after Zotatifin treatment were 97%, 87%, 70%, 83%, 37%, and 75%, respectively. Methods: Zotatifin (0.001 mg/kg-1 mg/kg, intravenous injection; 15 days) was used to treat mice bearing B-cell lymphoma xenograft models, and the tumor growth in vivo was observed. Results: Zotatifin inhibited the growth of B-cell lymphoma xenografts and was well tolerated in B-cell lymphoma xenograft models in vivo.
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• In Vitro:
  Methods: Zotatifin (0.0001 μM-1 μM, 72 hours) was used to treat MDA-MB-231 cells, and the antiproliferative activity was determined. Results: Zotatifin showed potent antiproliferative activity in MDA-MB-231 tumor cells, with a GI50 value of less than 15 nM. TMD8 and Pfeiffer DLBCL tumor cells were treated with Zotatifin (30 μM-100 μM, 3 or 24 hours), and the changes in protein levels were detected by WB. Results: Zotatifin reduced the expression of MYC, CCND3, BCL2, and MCL1 proteins in a time- and dose-dependent manner.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

eFT 226, eFT226, eFT-226, eIF4A, Zotatifin

Compound Identifiers

PubChem CID

129138801