In vitro study | TGR-1202 to PI3Kα, β, γ, δ, the selectivity of PI3Kδ is higher. TGR-1202 inhibits the proliferation of human whole blood CD19 cells with an IC50 in the range of 100-300 nM. Treatment of PBMC by TGR-1202(RP5264) will result in G2/M phase arrest followed by an increase in the number of cells in phase sub-G0. Cell viability experiments showed that the compound would cause significant growth inhibition of immortalized leukemia cells and primary leukemia cells, with inhibition of Akt phosphorylation. |