In vivo PK and cell IC50 coverage given as number of hours with plasma concentration above PI3Kα dependency in RAW cells or PI3Kδ dependency in JEKO cells cell IC50, corrected for protein in assay (RAW) and plasma protein binding
| PI3K | Dose/ schedule | Time above alpha 10x IC50 (h) | Time above beta 10x IC50 (h) | Time above delta 10xIC50 (h) | Time above gamma 10xIC50 (h) | |
|---|---|---|---|---|---|---|
| AZD8835 | α/δ | 50 mg/kg BD d1/d2 | 24 | 0 | 24 | 0 |
| PI-3065 | δ | 75 mg/kg QD | 0 | 0 | 22 | 0 |