Umbralisib hydrochloride

Umbralisib hydrochloride is a novel PI3Kδ inhibitor (IC50 and EC50 of 22.2 nM and 24.3 nM, respectively). Umbralisib hydrochloride is also active against CK1ε (EC50: 6.0 μM).

Umbralisib R-enantiomer (RP5264 R-enantiomer) is a delta inhibitor of PI3K and a less active enantiomer of TGR-1202. The IC50 of Umbralisib R-enantiomers against δPI3 kinase is at least 20 times lower than that of the inhibitors against other PI3K isoforms (A, β, and γ).

Umbralisib (TGR 1202) is a PI3Kδ inhibitor.

Umbralisib (TGR-1202) sulfate, an orally active compound, serves as a potent, selective inhibitor targeting both PI3Kδ and casein kinase-1-ε (CK1ε), with EC50 values of 22.2 nM and 6.0 μM, respectively. It demonstrates unique immunomodulatory effects on T cells in chronic lymphocytic leukemia (CLL) and is applicable in the research of hematological malignancies.

Umbralisib Tosylate (TGR-1202) is a potent, selectively dual inhibitor targeting PI3Kδ and casein kinase-1-ε (CK1ε), demonstrating oral activity. With EC50 values of 22.2 nM and 6.0 μM for PI3Kδ and CK1ε respectively, it shows unique immunomodulatory effects on T cells in chronic lymphocytic leukemia (CLL). This compound is utilized in the research of hematological malignancies.