TC ASK 10 (ASK1 Inhibitor 10) is a novel and potent apoptosis signal-regulating kinase 1 (ASK1) inhibitor ( IC50 = 14 nM).
Physicochemical Properties
| Molecular Formula | C21H23CL2N5O |
| Molecular Weight | 432.346222162247 |
| Exact Mass | 431.127 |
| CAS # | 1005775-56-3 |
| PubChem CID | 68661090 |
| Appearance | White to pink solid powder |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 3 |
| Rotatable Bond Count | 4 |
| Heavy Atom Count | 29 |
| Complexity | 525 |
| Defined Atom Stereocenter Count | 0 |
| InChi Key | IKKLFEDUYFZNBO-UHFFFAOYSA-N |
| InChi Code | InChI=1S/C21H21N5O.2ClH/c1-21(2,3)16-6-4-15(5-7-16)20(27)24-18-13-26-12-17(8-9-19(26)23-18)25-11-10-22-14-25;;/h4-14H,1-3H3,(H,24,27);2*1H |
| Chemical Name | 4-tert-butyl-N-(6-imidazol-1-ylimidazo[1,2-a]pyridin-2-yl)benzamide;dihydrochloride |
| 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
| ln Vitro | In INS-1 pancreatic β-cells, treatment with TC ASK 10 (Compound 10; 0–10 μM; 1 hour; INS-1 cells) at 0.3 μM suppresses the JNK that is produced by streptozotocin (STZ). Additionally, p38 phosphorylation is suppressed in a dose-dependent manner [1]. |
| ln Vivo | Rats were used in the pharmacokinetic profile testing. Oral bioavailability of TC ASK 10 (Compound 10·HCl; rat box at 0.1 mg/kg intravenously and 1 mg/kg orally) is good. For TC ASK 10, 0–8 hours, the Cmax, Tmax, and AUCpo are, respectively, 285.1 ng/mL, 1.67 h, and 275.4 ng.h/mL [1]. |
| Cell Assay |
Western Blot Analysis[1] Cell Types: INS-1 Cell Tested Concentrations: 0 μM, 0.3 μM, 1 μM, 3 μM, 10 μM Incubation Duration: 1 hour Experimental Results: Streptozotocin (STZ) found to inhibit streptozotocin (STZ) in INS- Induced JNK 1 pancreatic beta cells at a concentration of 0.3 μM. Phosphorylation of p38 was also inhibited in a dose-dependent manner. |
| References |
[1]. Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7326-9. |
Solubility Data
| Solubility (In Vitro) | DMSO : ~100 mg/mL (~231.29 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.78 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 (5.78 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 (5.78 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 | 2.3129 mL | 11.5647 mL | 23.1294 mL | |
| 5 mM | 0.4626 mL | 2.3129 mL | 4.6259 mL | |
| 10 mM | 0.2313 mL | 1.1565 mL | 2.3129 mL |