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Torin 2

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Chemical Structure| 1223001-51-1 同义名 : -
CAS号 : 1223001-51-1
货号 : A107433
分子式 : C24H15F3N4O
纯度 : 99%+
分子量 : 432.397
MDL号 : MFCD18782652
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 15 mg/mL(34.69 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+30% PEG300+water 1 mg/mL clear

PO 0.5% CMC-Na 35 mg/mL suspension

生物活性
靶点

  • mTOR

    mTOR, IC50:0.25 nM

  • ATM

    ATM, EC50:28 nM

  • ATR

    ATR, EC50:35 nM
描述 Torin 2 undergoes further profiling against a panel of lipid kinases, exhibiting IC50 values 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 demonstrates a 250 pM EC50 for inhibiting mTOR in cells while maintaining an 800-fold cellular selectivity compared to inhibition of PI3K and most other protein kinases[1]. Torin 2 demonstrates strong biochemical and cellular activity against PIKK family kinases, such as ATM (EC50 28 nM), ATR (EC50 35 nM), and DNA-PK (EC50 118 nM). Additionally, Torin 2 potently inhibits T308 of Akt, which is a direct substrate of PDK1 and an indirect substrate of PI3Ks, with an EC50 of less than 10 nM[2]. Torin 2 has the capability to inhibit both mTORC1 and mTORC2[4].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
human PC3 cells Function assay Inhibition of PI3Kalpha in human PC3 cells expressing Akt1 S473D mutant assessed as phosphorylation of Akt Thr308 by immunoblotting, EC50=0.2 μM 21322566
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.56mL

2.31mL

1.16mL

23.13mL

4.63mL

2.31mL
参考文献

[1]Liu Q, et al. Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer. J Med Chem. 2011 Mar 10;54(5):1473-80.

[2]Liu Q, et al. Characterization of Torin2, an ATP-competitive inhibitor of mTOR, ATM, and ATR. Cancer Res. 2013 Apr 15;73(8):2574-86.

[3]Codeluppi S, et al. Interleukin-6 secretion by astrocytes is dynamically regulated by PI3K-mTOR-calcium signaling. PLoS One. 2014 Mar 25;9(3):e92649.

[4]Wang X, et al. mTORC signaling in hematopoiesis. Int J Hematol. 2016 May;103(5):510-8.