PF-06843195 is a selective PI3Kα inhibitor, demonstrating potent activity with an IC50 of 18 nM in Rat1 fibroblasts and Kis for PI3Kα and PI3Kδ less than 0.018 nM and 0.28 nM, respectively, in biochemical kinase assays. It effectively suppresses the PI3K/mTOR signaling pathway and exhibits durable antitumor efficacy[1].

PI3Kα:0.018 nM (Ki), PI3Kα:18 nM (IC50, in Rat1 fibroblasts), PI3Kβ:360 nM (IC50, in Rat1 fibroblasts), PI3Kδ:0.28 nM (Ki), PI3Kδ:160 nM (IC50, in Rat1 fibroblasts)

PF-06843195 inhibits the proliferation of breast cancer cell lines MCF7 and T47D with IC50s of 62 nM and 32 nM, respectively, and pAKT (T308) in MCF7 and T47D cells with IC50s of 7.8 nM and 8.7 nM, respectively[1].

In rats, PF-06843195 can rapidly and quantitatively transform from PF-06862309[1]. PF-06843195 exhibits oral bioavailability (rat 25%) following oral administration (rat 10 mg/kg)[1]. PF-06843195 shows a moderate half-life (rat 3.6 h) due to high plasma clearance (30 mL/min/kg) combined with large volumes of distribution (3.0 L/kg) following intravenous administration (rat 2 mg/kg)[1].