Tenalisib (RP-6530) is a potent, selective, orally active p110δ/γ PI3K dual inhibitor with IC50 of 24.5 and 33.2 nM, respectively.
Tenalisib (RP-6530) displays good selectivity over p110α (>300-fold) and p110β (>100-fold) isoforms.
Tenalisib (RP-6530) inhibits LPS induced CD19+ cell proliferation in human whole blood with EC50 of 250 nM, and LPS induced CD45R+ cell proliferation in mouse whole blood with EC50 of 101 nM.
Tenalisib (RP-6530) shows the potential for treatment of cancer and inflammation diseases.
