PI3Kγ

9.1(pIC₅₀)

PI3Kα

5.1(pIC₅₀)

PI3Kβ

4.5(pIC₅₀)

PI3Kδ

6.5(pIC₅₀)

AZD3458 is a potent and remarkably selective PI3Kγ inhibitor with pIC50s of 9.1, 5.1,<4.5, and 6.5 for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively[1].

AZD3458 (Compound 15) also inhibits PI3KC2α, PI3KC2β, PI3KC2γ, and PI3KC3 with pIC50s of<5, 7.5, 5.5, and 5.1, respectively[1].

[1]. Pemberton N, et al. Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3-Kinase (PI3K)-γ Inhibitors. J Med Chem. 2018 Jun 28;61(12):5435-5441.