Physicochemical Properties
| Molecular Formula | C25H20F3N3O7 |
| Molecular Weight | 531.44 |
| CAS # | 2989537-78-0 |
| Related CAS # | QTX125;1279698-31-5 |
| Appearance | Off-white to gray 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
| Targets | HDAC6 |
| ln Vitro | QTX125 (82-48% hours; 25-500 nM) Annexin V/propidium iodide double staining and the cleavage of caspase-9, caspase-8, caspase-3, and PARP demonstrate that TFA administration causes subsequent apoptosis [1]. Using QTX125 TFA (10 nM, 10 μM, and 100 μM), MCL cell lines MINO, REC-1, IRM-2, and HBL-2 cells exhibit dose-dependent hyperacetylation of α-tubulin [1]. When it comes to Burkitt cell lymphoma, follicular lymphoma, and mantle cell lymphoma (MCL), QTX125 TFA exhibits the greatest growth inhibitory impact [1]. |
| ln Vivo | In nude mice xenografts of REC-1 or MINO cells, QTX125 TFA (60 mg/kg; i.p.; daily for 5 days; 4 weeks) therapy reduces tumor growth [1]. |
| Cell Assay |
Apoptosis Analysis[1] Cell Types: MINO, REC-1, IRM-2 and HBL-2 cells Tested Concentrations: 25 nM, 50 nM, 100 nM, 500 nM Incubation Duration: 24 hrs (hours), 48 hrs (hours) Experimental Results: Inhibited annexin V/propidium iodide double staining. Western Blot Analysis[1] Cell Types: MINO, REC-1, IRM-2 and HBL-2 cells Tested Concentrations: 25 nM, 50 nM, 100 nM, 500 nM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibited the cleavage of caspase-9, caspase-8, caspase-3, and PARP. |
| Animal Protocol |
Animal/Disease Models: Nude mice bearing REC-1 or MINO cells[1] Doses: 60 mg/kg Route of Administration: intraperitoneal (ip)administration; daily dosing for 5 days; for 4 weeks Experimental Results: Inhibited tumor growth in REC-1 or MINO cells xenografted in nude mice. |
| References |
[1]. In vitro and in vivo activity of a new small-molecule inhibitor of HDAC6 in mantle cell lymphoma. Haematologica. 2018 Nov;103(11):e537-e540. |
Solubility Data
| Solubility (In Vitro) |
DMSO :~125 mg/mL (~235.21 mM) H2O :< 0.1 mg/mL |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.91 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 20.8 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: ≥ 2.08 mg/mL (3.91 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 20.8 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8817 mL | 9.4084 mL | 18.8168 mL | |
| 5 mM | 0.3763 mL | 1.8817 mL | 3.7634 mL | |
| 10 mM | 0.1882 mL | 0.9408 mL | 1.8817 mL |