rel-Zotatifin (Synonyms: rel-eFT226)

Name: rel-Zotatifin
Brand: MedChemExpress
SKU: HY-112163A
Rating: 5.0 (1 reviews)

Cat. No.: HY-112163A Purity: 97.32%: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

rel-Zotatifin is the racemic isomer of Zotatifin, acts as an eIF4A inhibitor with activity less than Zotatifin. 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.

For research use only. We do not sell to patients.

rel-Zotatifin Chemical Structure

CAS No. : 2098191-54-7

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	Get quote
50 mg	Get quote

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Based on 1 publication(s) in Google Scholar

Other Forms of rel-Zotatifin:

Zotatifin Get quote

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Description

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]

Molecular Weight

487.56

Formula

C₂₈H₂₉N₃O₅

CAS No.

2098191-54-7

Appearance

Solid

Color

Off-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.[Relative stereochemistry]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 12.5 mg/mL (25.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0510 mL	10.2551 mL	20.5103 mL
5 mM	0.4102 mL	2.0510 mL	4.1021 mL
10 mM	0.2051 mL	1.0255 mL	2.0510 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)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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: ≥ 1.25 mg/mL (2.56 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (2.56 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.

Purity & Documentation

Purity: 97.32%

Select Batch:

Data Sheet (285 KB) SDS (251 KB)

COA (266 KB) LCMS (88 KB)

Handling Instructions (2659 KB)

References

[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	2.0510 mL	10.2551 mL	20.5103 mL	51.2757 mL
	5 mM	0.4102 mL	2.0510 mL	4.1021 mL	10.2551 mL
	10 mM	0.2051 mL	1.0255 mL	2.0510 mL	5.1276 mL
	15 mM	0.1367 mL	0.6837 mL	1.3674 mL	3.4184 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	2.0510 mL

rel-Zotatifin Related Classifications

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:

rel-Zotatifin2098191-54-7rel-eFT226Eukaryotic Initiation Factor (eIF)SARS-CoVApoptosisSARS coronavirusInhibitorinhibitorinhibit

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rel-Zotatifin (Synonyms: rel-eFT226)

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Other Forms of rel-Zotatifin:

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Complete Stock Solution Preparation Table

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