Zotatifin (Synonyms: eFT226)

Name: Zotatifin
Brand: MedChemExpress
SKU: HY-112163
Rating: 5.0 (9 reviews)

製品番号: HY-112163 純度: 99.69%: Data Sheet SDS COA 取扱説明書
FAQs
Technical Support

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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CAS 番号 : 2098191-53-6

容量	価格（税別）	在庫状況	数量
1 mg	$1350	在庫あり	Estimated Time of Arrival: December 31
2 mg	$2500	在庫あり	Estimated Time of Arrival: December 31
5 mg	$3800	在庫あり	Estimated Time of Arrival: December 31
10 mg	$5320	在庫あり	Estimated Time of Arrival: December 31
50 mg		お問い合わせ
100 mg		お問い合わせ

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Based on 9 publication(s) in Google Scholar

Other Forms of Zotatifin:

rel-Zotatifin 在庫あり

顧客検証

Cell Proliferation/Viability Assay

Bio/Physico-chemical Assay

In Vivo Efficacy Study

: 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.

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製品説明

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
MDA-MB-231	IC₅₀	1.5 1 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]
HAP1	IC₅₀	6.3 1 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	10.6 1 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 1 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	92 1 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]
MDA-MB-231	IC₅₀	218 1 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]
HAP1	IC₅₀	371 1 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]

体外実験

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.

体内実験

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.

臨床実験

分子量

487.55

分子式

C₂₈H₂₉N₃O₅

CAS 番号

2098191-53-6

Appearance

Solid

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

溶剤 & 溶解度

体外:

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 99.69%

Select Batch:

データシート (291 KB) SDS (254 KB)

COA (266 KB) HNMR (276 KB) LCMS (86 KB)

取扱説明書 (2659 KB)

参考文献

[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]

Complete Stock Solution Preparation Table

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

Zotatifin Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Zotatifin2098191-53-6eFT226eFT 226eFT-226Eukaryotic Initiation Factor (eIF)SARS-CoVApoptosisSARS coronavirusInhibitorinhibitorinhibit

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Zotatifin (Synonyms: eFT226)

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Other Forms of Zotatifin:

Zotatifin 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

生物活性

純度とドキュメンテーション

参考文献

カスタマーレビュー

Zotatifin 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Zotatifin Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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