eIF4A3-IN-8 is a selective ATP-competitive eukaryotic initiation factor (eIF4A3) inhibitor. eIF4A3-IN-8 can be used as a chemical probe to elucidate the specific functions of eIF4A3 and EJC (exon splicing complex).

Physicochemical Properties

Molecular Formula	C10H9NO2
Molecular Weight	175.1840
Exact Mass	175.063
CAS #	18474-59-4
PubChem CID	3163396
Appearance	Off-white to light brown solid powder
Density	1.3±0.1 g/cm3
Boiling Point	411.5±25.0 °C at 760 mmHg
Melting Point	220°C
Flash Point	202.7±23.2 °C
Vapour Pressure	0.0±1.0 mmHg at 25°C
Index of Refraction	1.696
LogP	2.77
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	2
Rotatable Bond Count	1
Heavy Atom Count	13
Complexity	217
Defined Atom Stereocenter Count	0
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

References

[1]. Discovery of selective ATP-competitive eIF4A3 inhibitors. Bioorg Med Chem. 2017 Apr 1;25(7):2200-2209.

Solubility Data

Solubility (In Vitro)

DMSO : ~100 mg/mL (~570.84 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (14.27 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (14.27 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (14.27 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	5.7084 mL	28.5421 mL	57.0841 mL
	5 mM	1.1417 mL	5.7084 mL	11.4168 mL
	10 mM	0.5708 mL	2.8542 mL	5.7084 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.