GSK3179106 is a potent, selective, and gut-restricted pyridone hinge binder small molecule RET kinase inhibitor with a RET IC50 of 0.3 nM and is efficacious in vivo. GSK3179106 is being developed by GlaxoSmithKline for the treatment of irritable bowel syndrome. GSK3179106 showed IC50s of 0.4 and 11 nM in the biochemical assay and cellular assay, respectively. GSK3179106 had a clean genotoxic profile with no embedded genotoxicity liabilities.
MedKoo Cat#: 555258
Name: GSK3179106
CAS#: 1627856-64-7
Chemical Formula: C22H21F4N3O4
Exact Mass: 467.1468
Molecular Weight: 467.42
Elemental Analysis: C, 56.53; H, 4.53; F, 16.26; N, 8.99; O, 13.69
| Solvent | mg/mL | mM | comments | |
|---|---|---|---|---|
| Solubility | ||||
| DMSO | 81.0 | 173.29 | ||
| DMSO:PBS (pH 7.2) (1:3) | 0.3 | 0.53 | ||
| Ethanol | 15.5 | 33.16 |
The following data is based on the product molecular weight 467.42 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
