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PF-06843195 is a highly selective PI3Kα inhibitor with an IC₅₀ of 18 nM in Rat1 fibroblasts. The K_is 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.

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

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).

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