PF-06843195 is a highly selective PI3Kα inhibitor with an IC 50 of 18 nM in Rat1 fibroblasts. The K i s of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy In Vitro PF-06843195 inhibits the breast cancer cell lines MCF7 and T47D proliferation with IC 50 s of 62 nM and 32 nM, respectively. PF-06843195 inhibits pAKT (T308) in MCF7 and T47D cells with IC 50 s of 7.8 nM and 8.7 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo In rats, PF-06843195 can rapidly and quantitatively transform from PF-06862309 . PF-06843195 exhibits oral bioavailability (rat 25 %) following oral administration (rat 10 mg/kg) . PF-06843195 exhibits 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) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Wistar Han Rats Dosage: 2 mg/kg (intravenous) and 10 mg/kg (oral gavage)(Pharmacokinetic Analysis) Administration: Intravenous (IV) or oral gavage (PO) Result: T 1/2 of 3.6 h for rats. Form:Solid IC50& Target:PI3Kα 18 nM (IC 50 , in Rat1 fibroblasts) PI3Kβ 360 nM (IC 50 , in Rat1 fibroblasts) PI3Kδ 160 nM (IC 50 , in Rat1 fibroblasts) PI3Kα 0.018 nM (Ki) PI3Kδ 0.28 nM (Ki)