Off target protein and potency: PI3Ka 136 nMPI3Kd 13.6 nMPI3Kg 47.8 nMDNA-PK 53.7 nMPI3K-C2b 54.1 nM
Potency assay (off target):
In Vitro kinase assay measurements against recombinant PI3Ks and PIKK using SelectScreen (Invitrogen)
Probe Selectivity in Vitro:
In Vitro kinase assay showed that AZD-6482 has 200-, 20-, and 70-fold selectivity over p110α, p110δ, and p110γ isoforms, respectively. Exhibit selectivity of approximately 80-fold over PI3K-C2 and DNA-PK and more than 1,000-fold over other PI3K-related kinases. profiling of AZD-6482 against a panel of 433 kinases using the KinomeScan approach (DiscoverX) showed that AZD-6482 is highly selective.