PI3K/mTOR Inhibitor-11 是一种具有口服活性的PI3K/mTOR抑制剂 (对 PI3Kα、PI3Kδ 和 mTOR 的IC50分别为 3.5、4.6 和 21.3 nM)。PI3K/mTOR Inhibitor-11 通过抑制 AKT 和 S6 蛋白的磷酸化来调节 PI3K/AKT/mTOR 信号通路。PI3K/mTOR Inhibitor-11 可用于癌症研究。
| 生物活性 | PI3K/mTOR Inhibitor-11 is an orally activePI3K/mTORinhibitor (IC50: 3.5, 4.6, and 21.3 nM forPI3Kα,PI3Kδ, and mTOR). PI3K/mTOR Inhibitor-11 regulates thePI3K/AKT/mTORsignaling pathway by inhibiting the phosphorylation ofAKTand S6 proteins. PI3K/mTOR Inhibitor-11 can be used in the research of cancers[1]. |
| IC50& Target[1] | PI3Kα 3.5 nM (IC50) | PI3Kδ 4.6 nM (IC50) | mTOR 21.3 nM (IC50) |
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体外研究
(In Vitro) | PI3K/mTOR Inhibitor-11 (compound 8o) inhibits various human cancer cell lines HT29, HCT15, H3122, HeLa, SW620, and H446 viability with IC50values of 0.25, 0.17, 0.29, 0.09, 0.16, and 0.97 μM, respectively[1].
PI3K/mTOR Inhibitor-11 (0-1.25 μM, 15 days) decreases the colony formation rates of HeLa and SW620 cells[1].
PI3K/mTOR Inhibitor-11 (0-2.5 μM, 24 h) arrests HeLa and SW620 cells at the G0/G1 phases[1].
PI3K/mTOR Inhibitor-11 (0-2.5 μM, 24 h) suppressees the phosphorylated AKT and S6 proteins in HeLa cells[1].
Apoptosis Analysis[1] | Cell Line: | HeLa and SW620 cells | | Concentration: | 0, 0.15625, 0.625, 1.25 μM | | Incubation Time: | 24 h | | Result: | Affected HeLa cells’ apoptosis rate from 6.10 to 66.04% in a dose-dependent manner. |
Western Blot Analysis[1] | Cell Line: | HeLa | | Concentration: | 0, 0.15625, 0.625, 1.25, 2.5 μM | | Incubation Time: | 24 h | | Result: | Suppressed the phosphorylated AKT (Ser473 and Thr308) and S6 proteins. |
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体内研究
(In Vivo) | PI3K/mTOR Inhibitor-11 (compound 8o, 15-60 mg/kg, intragastric administration) suppresses the growth of HeLa and SW620 xenograft tumors[1].
PI3K/mTOR Inhibitor-11 (1 mg/kg for i.v., 10 mg/kg for p.o., rats) shows oral bioavailability (76.81%)[1].
| Animal Model: | HeLa and SW620 xenograft models of female BALB/c nude mice[1]. | | Dosage: | 15, 30, and 60 mg/kg | | Administration: | Intragastric administration, daily for 30 days. | | Result: | The TGIs (tumor growth inhibitions): 80.22, 73.50, and 60.79% in the HeLa xenograft model at doses of 60, 30, and 15 mg/kg, respectively.
TGIs: 81.03, 70.81, and 60.58% in the SW620 xenograft model at doses of 60, 30, and 15 mg/kg, respectively. |
| Animal Model: | Rats[1]. | | Dosage: | 1 mg/kg for i.v., 10 mg/kg for p.o. | | Administration: | i.v., p.o. | | Result: | Pharmacokinetic parameters of PI3K/mTOR Inhibitor-11 (compound 8o)| dose (mg/kg) | T1/2(h) | Cmax(ng/mL) | CL (mL/min/kg) | F (%) | |
| 1 (i.v.) | | | 17.2 | | |
| 10 (p.o.) | 2.6 | 2995 | | 76.81% |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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