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- 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:
1223001-51-1
- 规格:
10 mM * 1 mL/1 mg/5 mg/10 mg/50 mg/100 mg/200 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥720.0 |
|---|---|---|---|
| 规格: | 1 mg | 产品价格: | ¥295.0 |
| 规格: | 5 mg | 产品价格: | ¥650.0 |
| 规格: | 10 mg | 产品价格: | ¥1100.0 |
| 规格: | 50 mg | 产品价格: | ¥3300.0 |
| 规格: | 100 mg | 产品价格: | ¥4900.0 |
| 规格: | 200 mg | 产品价格: | ¥8460.0 |
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Torin 2
CAS No. : 1223001-51-1
MCE 国际站:Torin 2
产品活性:Torin 2 是一种 mTOR 抑制剂,抑制细胞内 mTOR 活性,EC50 为 0.25 nM,比作用于 PI3K (EC50: 200 nM) 选择性高 800 倍。体外酶实验中,Torin 2 还抑制 DNA-PK,IC50 为 0.5 nM。Torin 2 抑制 mTORC1 和 mTORC2。
研究领域:PI3K/Akt/mTOR | Cell Cycle/DNA Damage | Autophagy | Apoptosis
作用靶点:mTOR | DNA-PK | Autophagy | Apoptosis
In Vitro: Torin 2 is subject to further profiling against a panel of lipid kinases with IC50s of 2.81 nM, 0.5 nM, 5.67 nM, 8.58 nM, 18.3 nM, 24.5 nM and 28.1 nM for mTOR, DNA-pK, p110γ, hVPS34, PI4Kβ, PI3K-C2β and PI3K-C2α, respectively. Torin 2 (Torin2) possesses a 250 pM EC50 for inhibiting mTOR in cells while maintaining 800-fold cellular selectivity relative to inhibition of PI3K and most other protein kinases. Torin 2 (Torin2) exhibits potent biochemical and cellular activity against PIKK family kinases including ATM (EC50 28 nM), ATR (EC50 35 nM) and DNA-PK (EC50 118 nM). Torin 2 potently inhibits T308 of Akt, a direct substrate of PDK1 and an indirect substrate of PI3Ks, with an EC50 of less than 10 nM. Torin-2 can suppress both?mTORC1 and mTORC2.
In Vivo: Torin 2 exhibits good bioavailability and exposure and can maintain strong inhibition of mTOR activity in lung and liver to at least six hours after a single dose of 20 mg/kg. Torin 2 is easier to produce on scale and exhibits improved pharmacokinetic properties which should enable it use in vivo experiments. Torin 2 strongly suppresses pS6K(T389) and p4EBP1(T37/46) and partly suppresses pAkt(T308). Treatment of mice with AZD6244 at 25 mg/kg results in a profound inhibition of pERK. Combined administration of Torin 2 (40 mg/kg) and AZD6244 (25 mg/kg) demonstrates strong inhibition of all pharmacodynamics markers. Treatment with Torin 2 and Rapamycin induces IL-6 secretion by astrocytes and may contribute to the reduction of mechanical hypersensitivity after SCI. Torin1 and Torin 2 treatment increases IL-6 mRNA, suggesting that the PI3K-mTOR pathway is a negative regulator of IL-6 expression in astrocytes. Importantly, Torin 2 treatment does not show any cell toxicity, as no signs of cell death are observed by TUNEL assay or by detection of cleaved-caspase 3 by western blotting.
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文献和实验【思路解读】一篇 10 分 SCI 文章,教你入手「铁死亡」的国自然课题设计思路
所介导,为确定「铁死亡」的发生是通过何靶点所调控,研究者利用了可抑制 mTORC1 活性的雷帕霉素类似物 Temsirolimus(CCI-779)进行实验,发现 CCI-779 可以使癌细胞对「铁死亡」敏感。 由于 CCI-779 和 mTOR 催化抑制剂 Torin 都可以恢复癌细胞对「铁死亡」的敏感性,研究者假设 mTORC1 而不是 mTORC2,负责具有 PI3K-AKT 通路突变癌细胞的抗性。 研究发现,短发夹 RNA 介导的 RAPTOR(mTORC1 的组成部分)沉默使 MDA
Development of ATP-Competitive mTOR Inhibitors
mTOR-mediated signaling. Therefore, numerous efforts have been initiated to develop ATP-competitive mTOR inhibitors that would block both mTORC1 and mTORC2 complex activity. Here, we describe our experimental approaches to develop Torin1 using a medium
相关专题 his method was successful in our lab using prostate tissue and for our specific objectives. Investigators must be aware that they will need to tailor the following protocol for their own research objectives
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