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).

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.