PI3K/mTOR Inhibitor-4 是一种泛 I 类 PI3K/mTOR 抑制剂，具有口服活性。PI3K/mTOR Inhibitor-4 对 PI3Kα、PI3Kγ、PI3Kδ 和 mTOR 具有酶抑制活性，IC₅₀ 值分别为 0.63 nM、22 nM、9.2 nM 和 13.85 nM。PI3K/mTOR Inhibitor-4 可用于癌症的研究。

PI3K/mTOR Inhibitor-4 is an orally active pan-class I PI3K/mTOR inhibitor. PI3K/mTOR Inhibitor-4 has enzymatic inhibition activity for PI3Kα, PI3Kγ, PI3Kδ and mTOR with IC 50 values of 0.63 nM, 22 nM, 9.2 nM and 13.85 nM, respectively. PI3K/mTOR Inhibitor-4 can be used for the research of cancer.

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PI3Kα 0.63 nM (IC50) PI3Kδ 9.2 nM (IC

PI3K/mTOR Inhibitor-4 (compound 8d-1) has enzymatic inhibition activity for PI3Kα, PI3Kδ, mTOR, PI3Kβ and PI3Kγ with IC50 values of 0.63 nM, 9.2 nM, 13.85 nM, 94.54 nM and 22 nM, respectively.
PI3K/mTOR Inhibitor-4 shows potent anti-proliferation activity in A549, Hela, HCT-116, HepG2, A375 and MCF-7 cells with IC50 values of 1.35 nM, 1.22 nM, 13.44 nM, 1.08 nM, 18.4 nM and 8.26 nM, respectively.
PI3K/mTOR Inhibitor-4 (2.5-10 μM; 24 h) inhibits the PI3K/AKT/mTOR pathway. has not independently confirmed the accuracy of these methods. They are for reference only.

PI3K/mTOR Inhibitor-4 (compound 8d-1) (i.v., oral; 1mg/kg, 10 mg/kg) displays favorable pharmacokinetic parameters in Sprague?Dawley rats.
PI3K/mTOR Inhibitor-4 (oral; 10-50 mg/kg) shows significant efficiency in Hela/A549 tumor xenograft models without causing significant weight loss and toxicity. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

[1]. Guoyi Yan, et al. Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors. Eur J Med Chem