AZD-6482

AZD-6482 is a potent and selective inhibitor of PI 3-kinase β (PI 3-Kβ) (IC₅₀ values are 0.69, 13.6, 47.8 and 136 nM for PI 3-Kβ, PI 3-Kδ, PI 3-Kγ and PI 3-Kα, respectively).  It displays 80-fold selectivity for PI3Kβ over PI3k-C2 and DNA-PK and more than 1,000-fold over other PI3K-related kinases. AZD6482 blocks Akt signaling and tumor growth in a large number of cancer cell lines, including those that are dependent on PI3Kβ activation or PTEN loss.