Selective PI3Kδ Inhibitor 1 Chemical Properties

storage temp. 

Store at -20°C

solubility 

DMSO: 43 mg/mL (100.13 mM);Ethanol: Insoluble

form 

Solid

color 

Off-white to gray

Water Solubility 

Water: Insoluble

Selective PI3Kδ Inhibitor 1 Usage And Synthesis

Uses

PI3Kδ-IN-5 (compound 7n) is a highly potent and selective inhibitor of PI3Kδ with an IC50 of 0.9 nM[1].

Biological Activity

Selective PI3Kδ Inhibitor 1 (compound 7n) is a PI3Kδ inhibitor with IC50 of 0.9 nM for PI3Kδ, which is more than 1000-fold selective for other class I PI3K isoforms. The IC50 values of it for PI3Kα/γ/β were 3670, 1460, and 21300 nM, respectively.

in vivo

Selective PI3Kδ Inhibitor 1 has favorable pharmacokinetic profile: good bioavailability and moderate in vivo half-life. In rats, its oral bioavailability was 41%; after intravenous injection, Vss, T _1/2 and CL were 2.8 L/kg, 3.4 h and 12 mL/min/kg, respectively .

target

References

[1] Terstiege I, et al. Discovery of triazole aminopyrazines as a highly potent and selective series of PI3Kδ inhibitors. Bioorg Med Chem Lett. 2017;27(3):679-687. DOI:10.1016/j.bmcl.2016.11.004