Physicochemical Properties
| CAS # | 2707510-30-1 |
| Appearance | White to off-white 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 |
| 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
| Targets | HSPA5 0.59 μM (IC50) |
| ln Vitro | GRP78-IN-3 (compound 8) is a strong small-molecule competitive inhibitor of Hsp70 substrate binding. In a spheroid tumor model (U251 glioblastoma cells and H520 lung cancer cells), GRP78-IN-3 (0.1-100 μM) exhibits more potent inhibitory effects[1]. |
| References |
[1]. Discovery and Development of a Selective Inhibitor of the ER Resident Chaperone Grp78. J Med Chem. 2022 Dec 14. |
Solubility Data
| Solubility (In Vitro) | DMSO : 5 mg/mL (14.60 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (1.46 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 5.0 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: ≥ 0.5 mg/mL (1.46 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 5.0 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.) |