Tenalisib 是一种新颖的，高效的，选择性的 PI3Kδ (IC50:25 nM) 和 PI3Kγ (IC50:33 nM) 抑制剂。

Tenalisib (RP6530) is a potent and selective inhibitor of PI3Kδ and PI3Kγ(IC50 values of 25 and 33 nM, respectively.)

In both HEL-RS and HEL-RR cells, Tenalisib exhibits modest proliferation inhibition (33-46% inhibition @ 10 μM). Addition of 10 μM 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 μM tenalisib, 4 h prior to the addition of ruxolitinib results in a significant reduction in EC50of ruxolitinib (5.8 μM) in HEL-RR cells.

Single agent(Tenalisib) activity is evident in difficult-to-treat subjects at ≥ 200 mg BID[2].

1639417-53-0

C23H18FN5O2

415.42

RP6530

DMSO:100 mg/mL (240.72 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years