pi3kδ in 8

PI3Kδ-IN-8 is a powerful and specific oral inhibitor of PI3Kδ, exhibiting an IC50 of 3.3 nM. It demonstrates preferential inhibition of PI3Kδ when compared to PI3Kα, PI3Kβ, and PI3Kγ, with IC50 values of 377.2 nM, 241.6 nM, and 17.9 nM, respectively. Furthermore, PI3Kδ-IN-8 possesses notable anti-tumor efficacy.

PI3Kα-IN-21 (compound 8) is a selective inhibitor of PI3Kα, demonstrating greater selectivity over PI3Kβ, PI3Kγ, and PI3Kδ by factors of 10.41, 16.99, and 37.53 respectively (IC50: 96.89 568.24 397.48 nM). This compound inhibits cancer cell activity, proliferation, and migration while inducing mitochondrial apoptosis through the PI3K Akt mTOR pathway. Additionally, PI3Kα-IN-21 has shown in vivo antitumor efficacy in a mouse model of non-small cell lung cancer.