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PI3K/mTOR Inhibitor-4

CAS No. : 2361215-32-7

MCE 站：PI3K/mTOR Inhibitor-4

产品活性：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。

研究领域：PI3K/Akt/mTOR

作用靶点：PI3K  |  mTOR

In Vitro: 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 M; 24 h) inhibits the PI3K/AKT/mTOR pathway.

In Vivo: PI3K/mTOR Inhibitor-4 (compound 8d-1) (i.v., oral; 1mg/kg, 10 mg/kg) displays favorable pharmacokinetic parameters in SpragueDawley 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.

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