(Rac)-JBJ-04-125-02 acetate is the racemate of JBJ-04-125-02, a potent, mutant-selective, allosteric and orally active EGFR inhibitor.

Physicochemical Properties

Molecular Formula	C29H26FN5O3S.1/3C2H4O2
Molecular Weight	563.63
Appearance	Solid powder
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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
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]. Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor. Cancer Discov. 2019 Jul;9(7):926-943.

Solubility Data

Solubility (In Vitro)

DMSO : 100 mg/mL (177.42 mM; with sonication)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (4.44 mM)(Saturation unknown) in 10% DMSO 40% PEG300 5% Tween-80 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, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix well; then add 50 μL Tween-80 to the above system and mix well; then add 450 μL saline to make it 1 mL. *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.7742 mL	8.8711 mL	17.7421 mL
	5 mM	0.3548 mL	1.7742 mL	3.5484 mL
	10 mM	0.1774 mL	0.8871 mL	1.7742 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.