tenalisib-r-enantiomer

Description: Tenalisib R Enantiomer is the R enantiomer of Tenalisib (also known as RP6530). Tenalisib is a new, potent and selective dual PI3Kdelta/gamma inhibitor with IC50 of 24.5 nM and 33.2 nM for PI3Kdelta and PI3Kgamma, respectively. It displays selective for PI3Kdelta/gamma with selectivity over alpha and beta isoforms of more than 300-fold and 100-fold, respectively. Tenalisib exhibits modest proliferation inhibition (33-46% inhibition at 10 uM) in both HEL-RS and HEL-RR cells. Addition of 10 uM tenalisib to ruxolitinib is synergistic resulting in a near-complete inhibition of proliferation (> 90% for HEL-RS and > 70% for HEL-RR). Addition of 5 uM tenalisib, 4 h prior to the addition of ruxolitinib results in a significant reduction in EC50of ruxolitinib (5.8 uM) in HEL-RR cells.

References: Blood 2015 126:1495