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PF-06843195

CAS No. : 2067281-51-8

MCE 国际站：PF-06843195

产品活性：PF-06843195 是一种高度选择性的 PI3Kα 抑制剂，在 Rat1 成纤维细胞中，其 IC₅₀ 为 18 nM。PF-06843195 作用于 PI3Kα 和 PI3Kδ 的 K_i 分别小于 0.018 nM 和 0.28 nM。PF-06843195对 PI3K/mTOR 信号通路有明显抑制作用，且具有持久的抗肿瘤作用。

研究领域：PI3K/Akt/mTOR

作用靶点：PI3K

In Vitro: 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 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).

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