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。
| 生物活性 | PI3K/mTOR Inhibitor-4 is an orally active pan-class IPI3K/mTORinhibitor. PI3K/mTOR Inhibitor-4 has enzymatic inhibition activity forPI3Kα,PI3Kγ,PI3KδandmTORwithIC50values of 0.63 nM, 22 nM, 9.2 nM and 13.85 nM, respectively. PI3K/mTOR Inhibitor-4 can be used for the research ofcancer[1]. |
| IC50& Target[1] | PI3Kα 0.63 nM (IC50) | PI3Kδ 9.2 nM (IC50) | mTOR 13.85 nM (IC50) | PI3Kβ 94.54 nM (IC50) | PI3Kγ 22 nM (IC50) |
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体外研究
(In Vitro) | PI3K/mTOR Inhibitor-4 (compound 8d-1) has enzymatic inhibition activity for PI3Kα, PI3Kδ, mTOR, PI3Kβ and PI3Kγ with IC50values of 0.63 nM, 9.2 nM, 13.85 nM, 94.54 nM and 22 nM, respectively[1].
PI3K/mTOR Inhibitor-4 shows potent anti-proliferation activity in A549, Hela, HCT-116, HepG2, A375 and MCF-7 cells with IC50values of 1.35 nM, 1.22 nM, 13.44 nM, 1.08 nM, 18.4 nM and 8.26 nM, respectively[1].
PI3K/mTOR Inhibitor-4 (2.5-10 μM; 24 h) inhibits the PI3K/AKT/mTOR pathway[1].
Cell Viability Assay[1] | Cell Line: | PC12 and LO2 cells | | Concentration: | 0.625-20 μM | | Incubation Time: | 72 h | | Result: | Showed low toxicity in concentrations from 0.625 μM to 20 μM. |
Western Blot Analysis[1] | Cell Line: | Hela cells | | Concentration: | 2.5, 5 and 10 μM | | Incubation Time: | 24 h | | Result: | Dose-dependently decreased the level of phosphorylation of AKT and its downstream target S6 in Hela cell line. |
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体内研究
(In Vivo) | PI3K/mTOR Inhibitor-4 (compound 8d-1) (i.v., oral; 1mg/kg, 10 mg/kg) displays favorable pharmacokinetic parameters in Sprague–Dawley rats[1].
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[1].
| Animal Model: | SD rats (male; 200-220 g)[1] | | Dosage: | 1, 10 mg/kg | | Administration: | Intravenous, oral | | Result: | | IV (1 mg/kg) | PO (10 mg/kg) | | CL (ml/min/kg) | Vss (ml/kg) | Tmax(h) | Cmax(ng/ml) | AUCinf (ng*h/ml) | t1/2(h) | F(%) | | 8.6 | 1199.81 | 2.67 | 886.67 | 4753.35 | 1.78 | 24.1 |
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| Animal Model: | BALB/c nude mice (female; 6-7 weeks; 18-22 g)[1] | | Dosage: | 10, 20, 40, 50 mg/kg/d (Hela model) and 20, 40 mg/kg/d (A549 model) | | Administration: | Oral | | Result: | Inhibited the growth of xenograft tumors in a dose-dependent manner. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
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