Cat. No.: HY-112163

Zotatifin

(Synonyms: eFT226)

10 Cited Publications

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Based on 10 publication(s) in Google Scholar

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 (IC₅₀=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 (IC₉₀=37 nM). Zotatifin induces cell apoptosis.

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Pureté: 99.69%
CAS No.: 2098191-53-6
Formule: C₂₈H₂₉N₃O₅
Masse moléculaire:487.55

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Zotatifin Chemical Structure

CAS No.: 2098191-53-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (10)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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 (IC₅₀=2 nM) and interferes with the assembly of the eIF4F initiation complex^[1]. Zotatifin shows robust antiviral effects, it effectively reduces viral infectivity by inhibiting SARS-CoV-2 NP protein biogenesis (IC₉₀=37 nM)^[2]. Zotatifin induces cell apoptosis^[1].

IC₅₀ & Target

eIF4

Cellular Effect

Cell Line	Type	Value	Description	References
HAP1	IC₅₀	371 nM Compound: (-)-eFT226	Inhibition of eIF4A1 F163L mutant in human HAP1 cells assessed as reduction in cell proliferation incubated for 72 hrs by CellTiter-Glo reagent based assay Inhibition of eIF4A1 F163L mutant in human HAP1 cells assessed as reduction in cell proliferation incubated for 72 hrs by CellTiter-Glo reagent based assay	[PMID: 32470302]
HAP1	IC₅₀	6.3 nM Compound: (-)-eFT226	Inhibition of eIF4A1 in human HAP1 cells assessed as reduction in cell proliferation incubated for 72 hrs by CellTiter-Glo reagent based assay Inhibition of eIF4A1 in human HAP1 cells assessed as reduction in cell proliferation incubated for 72 hrs by CellTiter-Glo reagent based assay	[PMID: 32470302]
MDA-MB-231	IC₅₀	1.5 nM Compound: (-)-eFT226	Inhibition of eIF4A1 in human MDA-MB-231 cells assessed as inhibition of cellular-translation incubated for 4 hrs by specific tandem sequence motif repeat AGAGAG in 5'- UTR containing luciferase reporter gene assay Inhibition of eIF4A1 in human MDA-MB-231 cells assessed as inhibition of cellular-translation incubated for 4 hrs by specific tandem sequence motif repeat AGAGAG in 5'- UTR containing luciferase reporter gene assay	[PMID: 32470302]
MDA-MB-231	IC₅₀	10.6 nM Compound: (-)-eFT226	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell proliferation incubated for 72 hrs by CellTiter-Glo reagent based assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell proliferation incubated for 72 hrs by CellTiter-Glo reagent based assay	[PMID: 32470302]
MDA-MB-231	IC₅₀	13.8 nM Compound: (-)-eFT226	Inhibition of eIF4A1 in human MDA-MB-231 cells assessed as inhibition of cellular-translation incubated for 4 hrs by specific tandem sequence motif repeat GGCGGC in 5'- UTR containing luciferase reporter gene assay Inhibition of eIF4A1 in human MDA-MB-231 cells assessed as inhibition of cellular-translation incubated for 4 hrs by specific tandem sequence motif repeat GGCGGC in 5'- UTR containing luciferase reporter gene assay	[PMID: 32470302]
MDA-MB-231	IC₅₀	218 nM Compound: (-)-eFT226	Inhibition of eIF4A1 in human MDA-MB-231 cells assessed as inhibition of cellular-translation incubated for 4 hrs by specific tandem sequence motif repeat CAACAA in 5'- UTR containing luciferase reporter gene assay Inhibition of eIF4A1 in human MDA-MB-231 cells assessed as inhibition of cellular-translation incubated for 4 hrs by specific tandem sequence motif repeat CAACAA in 5'- UTR containing luciferase reporter gene assay	[PMID: 32470302]
MDA-MB-231	IC₅₀	92 nM Compound: (-)-eFT226	Inhibition of eIF4A1 in human MDA-MB-231 cells assessed as inhibition of cellular-translation incubated for 4 hrs by specific tandem sequence motif repeat CCGCCG in 5'- UTR containing luciferase reporter gene assay Inhibition of eIF4A1 in human MDA-MB-231 cells assessed as inhibition of cellular-translation incubated for 4 hrs by specific tandem sequence motif repeat CCGCCG in 5'- UTR containing luciferase reporter gene assay	[PMID: 32470302]

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^[1].
Zotatifin inhibits in vitro translation as a sequence-dependent manner, the IC₅₀ 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^[1].
Zotatifin (0.0001 μM-1 μM; 72 hours) inhibits tumor cells growth as a dose-dependent manner. It shows a potent anti-proliferative activity (GI₅₀<15 nM) in MDA-MB-231 tumor cells, but eIF4A1 F163L mutation rescues eFT226 anti-proliferative activity^[1].
Zotatifin (0.0001 μM-1 μM; 72 hours) inhibits tumor cell growth, exhibits GI₅₀ values for TMD8, SU-DHL-2, HBL1, Pfeiffer, SU-DHL-6, SU-DHL-10, VAL, Carnaval, U2973, Ramos, Jeko1, Mino, and Rec-1 cells are 4.1 nM, 3 nM, 5.6 nM, 3.7 nM, 5.3 nM, 7.3 nM, 6.6 nM, 4.4 nM, 4.2 nM, 4.6 nM, 7.9 nM, 11.2 nM and 11.8 nM, respectively^[1].
Zotatifin (30 μM-100 μM; 3 or 24 hours) results in translational regulation of oncogenic protein, decreases MYC,CCND3,BCL2 and MCL1 protein expression as a time- and dose-dependent manner^[1].
The anti-viral activity of Zotatifin is demonstrated by various assays: such as TCID50 assay, Plaque assay, NP-staining assay, et al^[2].
Zotatifin (10 nM, 100 nM, 200 nM, 500 nM, 2 μM, 10 μM; 1 or 2 hours pre-treatment before virus isolates) decreases the detection of the viral NP protein and reduces viral infectivity in a concentration-dependent matter in Vero E6 cells cells infected with SARS-CoV-2 isolates^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

MDA-MB-231 tumor cells
Concentration:

0.0001 μM, 0.001 μM, 0.01 μM, 0.1 μM, 1 μM
Incubation Time:

72 hours
Result:

Inhibited cell growth with a GI₅₀ of 15 nM, and F163L mutant rescued anti-proliferative effects.

Cell Proliferation Assay^[1]

Cell Line:

DLBCL-ABC; DLBCL-GCB; Burkitt; and MCL tumor type cells
Concentration:

0.0001 μM, 0.001 μM, 0.01 μM, 0.1 μM, 1 μM
Incubation Time:

72 hours
Result:

Inhibited cell growth with GI₅₀ values ranging from 3 nM to 20 nM.

Cell Proliferation Assay^[1]

Cell Line:

TMD8 and Pfeiffer DLBCL tumor cells
Concentration:

30 μM; 100 μM
Incubation Time:

3 or 24 hours
Result:

Decreased MYC, CCND3, Bcl2,and MCL1 protein levels.

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^[1].
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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

B-cell lymphoma xenograft model^[1]
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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 2098191-53-6
Appearance Solid
Masse moléculaire 487.55
Formule C₂₈H₂₉N₃O₅
Color White to light yellow
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
Synonyms

eFT226
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (10)

All Cell Proliferation/Viability AssayBio/Physico-chemical AssayIn Vivo Efficacy Study

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Journal Impact Factor

Nat Methods

Decoding post-transcriptional regulatory networks by RNA-linked CRISPR screening in human cells. [Abstract]

2025 Jun;22(6):1237-1246. PMID: 40442371
J Clin Invest

Co-targeting a MYC-eIF4A survival axis improves the efficacy of KRAS inhibitors in lung cancer. [Abstract]

2023 Aug 15;133(16):e167651. PMID: 37384411

Zotatifin purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2023 Aug 15;133(16):e167651. [Abstract]

Zotatifin (eFT226; eIF4Ai) (25 nM; 72 h) potently sensitized 75% of the NSCLC cell lines to KRAS G12C inhibitors, resulting in the loss of approximately 60%-90% of cells within just 3 days.

Zotatifin purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2023 Aug 15;133(16):e167651. [Abstract]

Long-term cell proliferation assay of KRAS-mutant NSCLC cells treated with Zotatifin (eFT226; eIF4Ai) (25 nM; 3 weeks).

Zotatifin purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2023 Aug 15;133(16):e167651. [Abstract]

Caspase-3/7 activity in sensitive H23 and H1573 cell lines in response to Zotatifin (eFT226; eIF4Ai) (25 nM; 120 h).

Zotatifin purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2023 Aug 15;133(16):e167651. [Abstract]

The graphs depicted the fold change in tumor volume of KRAS G12C-mutant xenograft mice treated with Zotatifin (eFT226; eIF4Ai) (0.5 mg/kg; i.p.; once every 4 days for 28 d).

Zotatifin purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2023 Aug 15;133(16):e167651. [Abstract]

Percentage live/dead of high MYC (DFCI-730, DFCI-456, MGH-9029-1B) PDOTSs treated with Zotatifin (eFT226; eIF4Ai) (25 nM; 6 d) in 3D microfluidic culture.
Oncogene

RBM12 drives PD-L1-mediated immune evasion in hepatocellular carcinoma by increasing JAK1 mRNA translation. [Abstract]

2024 Oct;43(41):3062-3077. PMID: 39187545
Cell Rep

Proteomics reveal cap-dependent translation inhibitors remodel the translation machinery and translatome. [Abstract]

2021 Oct 12;37(2):109806. PMID: 34644561
Pharmaceuticals (Basel)

In Vitro Safety, Off-Target and Bioavailability Profile of the Antiviral Compound Silvestrol. [Abstract]

2022 Aug 31;15(9):1086. PMID: 36145307
Int J Mol Sci

eIF4A1 Is a Prognostic Marker and Actionable Target in Human Hepatocellular Carcinoma. [Abstract]

2023 Jan 20;24(3):2055. PMID: 36768380
Viruses

Rocaglates as Antivirals: Comparing the Effects on Viral Resistance, Anti-Coronaviral Activity, RNA-Clamping on eIF4A and Immune Cell Toxicity. [Abstract]

2022 Mar 3;14(3):519. PMID: 35336926
bioRxiv

Co-Targeting Nuclear Export and Translation Initiation Uncovers a Therapeutic Vulnerability in Lethal Prostate Cancer. [Abstract]

2026 May 7:2026.05.04.722693. PMID: 42146671
bioRxiv

2025 Nov 18.
bioRxiv

Combined HDAC and eIF4A inhibition: A novel epigenetic therapy for pancreatic adenocarcinoma. [Abstract]

2024 Jul 2:2024.06.30.600495. PMID: 39005268

Solvant et solubilité

In Vitro:

DMSO : ≥ 100 mg/mL (205.11 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0511 mL

10.2554 mL

20.5107 mL

5 mM

0.4102 mL

2.0511 mL

4.1021 mL

10 mM

0.2051 mL

1.0255 mL

2.0511 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.13 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.5 mg/mL (5.13 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
Elemental Analysis Report (2659 KB)
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IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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.

[2]. Gordon DE, et al. A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.Nature. 2020 Apr 30. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0511 mL	10.2554 mL	20.5107 mL	51.2768 mL
	5 mM	0.4102 mL	2.0511 mL	4.1021 mL	10.2554 mL
	10 mM	0.2051 mL	1.0255 mL	2.0511 mL	5.1277 mL
	15 mM	0.1367 mL	0.6837 mL	1.3674 mL	3.4185 mL
	20 mM	0.1026 mL	0.5128 mL	1.0255 mL	2.5638 mL
	25 mM	0.0820 mL	0.4102 mL	0.8204 mL	2.0511 mL
	30 mM	0.0684 mL	0.3418 mL	0.6837 mL	1.7092 mL
	40 mM	0.0513 mL	0.2564 mL	0.5128 mL	1.2819 mL
	50 mM	0.0410 mL	0.2051 mL	0.4102 mL	1.0255 mL
	60 mM	0.0342 mL	0.1709 mL	0.3418 mL	0.8546 mL
	80 mM	0.0256 mL	0.1282 mL	0.2564 mL	0.6410 mL
	100 mM	0.0205 mL	0.1026 mL	0.2051 mL	0.5128 mL

Keywords

Zotatifin

10 Cited Publications

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Zotatifin

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) Zotatifin

Activité biologique

Chemical Information

Publications (10)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Zotatifin

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) Zotatifin

Activité biologique

Chemical Information

Publications (10)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Zotatifin Related Classifications

HY-112163 Related Classifications