Art. -Nr.: HY-112163A

rel-Zotatifin

(Synonyms: rel-eFT226)

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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.

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Reinheit: 97.32%
CAS. Nr.: 2098191-54-7
Formel: C₂₈H₂₉N₃O₅
Molecular Weight:487.56

Speicherung:

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

rel-Zotatifin Chemical Structure

CAS. Nr.: 2098191-54-7

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Biologische Aktivität
- Beschreibung
- Cellular Effect
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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]

Chemical Information

CAS. Nr. 2098191-54-7
Appearance Solid
Molecular Weight 487.56
Formel C₂₈H₂₉N₃O₅
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]
Synonyms

rel-eFT226
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

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)

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

2.0510 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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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: ≥ 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.

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 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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	2.0510 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

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rel-Zotatifin

MCE Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

rel-Zotatifin Related Classifications

HY-112163A Related Classifications