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- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1207358-59-5
- 规格：
10 mM * 1 mL/2 mg/5 mg/10 mg/50 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1723.0 |
|---|---|---|---|
| 规格： | 2 mg | 产品价格： | ￥620.0 |
| 规格： | 5 mg | 产品价格： | ￥1650.0 |
| 规格： | 10 mg | 产品价格： | ￥2300.0 |
| 规格： | 50 mg | 产品价格： | ￥5700.0 |
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mTOR inhibitor-3
CAS No. : 1207358-59-5
MCE 国际站：mTOR inhibitor-3
产品活性：mTOR inhibitor-3 是一种有效的 mTOR 抑制剂，Ki 值为 1.5 nM。mTOR inhibitor-3 在细胞实验及体内药代动力学 (PK)/药效学 (PD) 实验中都抑制 mTORC1 和 mTORC2。
研究领域：PI3K/Akt/mTOR
作用靶点：mTOR
In Vitro: mTOR inhibitor-3 (Compound 12i) inhibits mTOR with a Ki of 1.5 nM, 500-fold selectivity over closely related PI3 kinases. mTOR inhibitor-3 inhibits NCI-PC3 and MCF7neo/Her2 cells proliferation with IC50s of 150 nM and 57 nM, respectively.
In Vivo: mTOR inhibitor-3 (Compound 8h) has high free plasma clearance in both mice (1818 mL/min/kg) and rats (1538 mL/min/kg in rat) . mTOR inhibitor-3 (Compounds 12i) is selected for this study due to its potency, selectivity, and favorable mouse PK profile. Plasma levels of mTOR inhibitor-3 6 h following oral administration in PC3 tumor-bearing mice along with the fold decreases of phosphorylated mTORC1 and -2 substrates relative to time-matched vehicle controls. mTOR inhibitor-3 has moderate terminal elimination half-life (t1/2=1.7 h for mouse(1 mg/kg, iv)). mTOR inhibitor-3 achieves tumor stasis at the highest 200 mg/kg/day dose examined, which appears to also be approaching the limit of tolerability for this molecule.
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文献和实验The senescence program is activated in response to diverse stress stimuli potentially compromising genetic stability and leads to an irreversible cell cycle arrest. The mTOR pathway plays a crucial role in the regulation of cell metabolism
The adaptive response to hypoxia, low oxygen tension, involves inhibition of energy-intensive cellular processes including protein translation. This effect is mediated in part through a decrease in the kinase activity of mammalian target
The mammalian target of rapamycin (mTOR) is the catalytic subunit of two multiprotein complexes, mTOR complex-1 (mTORC1) and mTOR complex-2 (mTORC2). Clinically used rapamycin and rapalogs are FKBP12-dependent allosteric inhibitors of mTORC
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