Molecular Formula | C31H24F3N5O3 |
Molar Mass | 571.55 |
Solubility | 10 mM in DMSO |
Storage Condition | -20℃ |
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. |
In vivo study | TGR-1202(RP5264) in rodents, has good oral absorption capacity, favorable pharmacokinetic properties. In vivo safety was good. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.75 ml | 8.748 ml | 17.496 ml |
5 mM | 0.35 ml | 1.75 ml | 3.499 ml |
10 mM | 0.175 ml | 0.875 ml | 1.75 ml |
5 mM | 0.035 ml | 0.175 ml | 0.35 ml |