Catalog No.S8194 Synonyms: Rp-5264
Molecular Weight(MW): 571.55
TGR-1202, a novel, next generation PI3Kδ inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 & 24.3 nM, respectively.
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|Description||TGR-1202, a novel, next generation PI3Kδ inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 & 24.3 nM, respectively.|
The compound displays a high degree of selectivity over the alpha (>1000 fold), beta (>30-50 fold), and gamma (>15-50 fold) isoforms. Additionally, the compound causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM. Treatment of PBMC with RP5264 results initially in a G2/M arrest followed by subsequent increase in the number of Sub G0 cells. Viability assays demonstrate that the compound causes a significant inhibition in growth as well as Akt phosphorylation of immortalized and primary leukemic cells.
|In vivo||The compound exhibits good oral absorption with favourable pharmacokinetic properties in rodents. It also has an excellent safety profile.|
|In vitro||DMSO||100 mg/mL warmed (174.96 mM)|
|Ethanol||7 mg/mL warmed (12.24 mM)|
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