| Description | TGFβRI-IN-2 is a selective, potent and orally active inhibitor of (Activin-Like Kinase 5) ALK 5(pIC50 and pEC50 values of 7.6 and 6.63, respectively). |
| In vitro | Umbralisib R-enantiomer exhibits IC50 with respect to the δ type PI3-kinase that is at least 20-fold lower than the inhibitor's IC50 with respect to the rest of the other PI3K isoforms (i.e., a, β, and γ). |
| In vivo | TGFβRI-IN-2 oral administation with 50, 150 and 500 mg/kg and 5 days induces cardiovascular toxicity characterized by valvular interstitial cell proliferation, neutrophil presence, hemorrhage and fibrin deposition in the heart valves. |
| Target activity | ALK5: |
| Synonyms | TGFβRI-IN-2 |
| molecular weight | 411.82 |
| Molecular formula | C20H15ClFN5O2 |
| CAS | 1976038-41-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Wang H, et al. Design, synthesis and optimization of novel Alk5 (activin-like kinase 5) inhibitors.Bioorg Med Chem Lett. 2016 Sep 1;26(17):4334-9. |