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PI3K/mTOR Inhibitor-12
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PI3K/mTOR Inhibitor-12图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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)

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.
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.
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
ParameterI.V. (1 mg/kg)ParameterP.O. (5 mg/kg)
T1/2(h)0.6T1/2(h)2.33
CL (mL/h/kg)1428Cmax(ng/mL)1218
Vdss (mL/Kg)528AUC0-∞(h*ng/mL)1356
AUC0-∞(h*ng/mL)760F%33.1
分子量

611.62

Formula

C27H27F2N9O4S

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.