PI3K/mTOR Inhibitor-12 是一种口服有效的选择性PI3K/mTOR抑制剂，对 PI3Kα 和 mTOR 的IC50值分别为 0.06 nM 和 3.12 nM。PI3K/mTOR Inhibitor-12 具有抗肿瘤活性。PI3K/mTOR Inhibitor-12 具有较低的肝毒性。
| 生物活性 | PI3K/mTOR Inhibitor-12 is a potent, orally active and selectivePI3K/mTORinhibitor withIC50values of 0.06 nM and 3.12 nM forPI3KαandmTOR, respectively. PI3K/mTOR Inhibitor-12 has antitumor activity. PI3K/mTOR Inhibitor-12 has lower liver toxicity[1]. |
| IC50& Target[1] | PI3Kα 0.06 nM (IC50) | mTOR 3.12 nM (IC50) |
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体外研究
(In Vitro) | PI3K/mTOR Inhibitor-12 (compound 48; 72 h) 抑制癌细胞生长，对 PC-3、HT-29、HCT116、LOVO 和 HUVEC 细胞 的 IC50值分别为 0.07、0.09、0.54、0.54 和 0.68 μM[1].
PI3K/mTOR Inhibitor-12 (0.25-1 μM; 12-48 h; HCT116 和 HT-29 细胞) 抑制细胞环境中 PI3K 和 mTOR 的激活[1]。
Western Blot Analysis[1] | Cell Line: | HCT116 and HT-29 cells | | Concentration: | 0.25, 0.5, and 1 μM | | Incubation Time: | 12, 24, and 48 hours | | Result: | Inhibited the expression levels of AKT, p70S6K and their phosphorylated forms in a dose- and time-dependent manner. |
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体内研究
(In Vivo) | PI3K/mTOR Inhibitor-12 (compound 48; 20 mg/kg; p.o.; 每日一次, 持续 14 天) 抑制雌性 BALB/c 裸鼠中 HCT116 异种移植物的肿瘤生长[1]。
PI3K/mTOR Inhibitor-12 (1 和 5 mg/kg; i.v. 和 p.o.; 雄性 SD 大鼠) 具有快速血浆清除率 (1428 mL/h/kg) 和短 T1/2(2.33 h)，AUC0-∞为 1356 h*ng/mL[1]。
| Animal Model: | HCT116 xenografts in female BALB/c nude mice[1] | | Dosage: | 20 mg/kg | | Administration: | Oral administration, daily, for 14 days | | Result: | Reduced the growth of HCT116 tumors, and the tumor growth inhibition (TGI) was 73.33%.
Had lower liver toxicity of HCT116 xenografts in female BALB/c nude mice.
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| Animal Model: | Male SD rats[1] | | Dosage: | 1 and 5 mg/kg | | Administration: | Intravenous injection (1 mg/kg) and oral administration (5 mg/kg) | | Result: | 1.19| Parameter | I.V. (1 mg/kg) | Parameter | P.O. (5 mg/kg) | | T1/2(h) | 0.6 | T1/2(h) | 2.33 | | CL (mL/h/kg) | 1428 | Cmax(ng/mL) | 1218 | | Vdss (mL/Kg) | 528 | AUC0-∞(h*ng/mL) | 1356 | | AUC0-∞(h*ng/mL) | 760 | F% | 33.1 |
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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. |
