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Torin 2
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。
Torin 2图片
CAS NO:1223001-51-1
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议
1 g电议

产品介绍
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-PKIC50为 0.5 nM。Torin 2 抑制mTORC1mTORC2
生物活性

Torin 2 is anmTORinhibitor withEC50of 0.25 nM for inhibiting cellularmTORactivity, and exhibits 800-fold selectivity overPI3K(EC50: 200 nM). Torin 2 also inhibitsDNA-PKwith anIC50of 0.5 nM in the cell free assay. Torin 2 can suppress bothmTORC1andmTORC2.

IC50& Target[1][4]

mTOR

2.81 nM (IC50)

mTOR

0.25 nM (EC50, Cell Assay)

mTORC1

 

mTORC2

 

DNA-PK

0.5 nM (IC50)

PI3K-C2α

28.1 nM (IC50)

PI3K-C2β

24.5 nM (IC50)

p110γ

5.67 nM (IC50)

hVps34

8.58 nM (IC50)

ΡΙ4Κβ

18.3 nM (IC50)

Autophagy

 

PI3K

200 nM (EC50, Cell Assay)

体外研究
(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 EC50for inhibiting mTOR in cells while maintaining 800-fold cellular selectivity relative to inhibition of PI3K and most other protein kinases[1]. Torin 2 (Torin2) exhibits potent biochemical and cellular activity against PIKK family kinases including ATM (EC5028 nM), ATR (EC5035 nM) and DNA-PK (EC50118 nM). Torin 2 potently inhibits T308 of Akt, a direct substrate of PDK1 and an indirect substrate of PI3Ks, with an EC50of less than 10 nM[2]. Torin-2 can suppress both mTORC1 and mTORC2[4].

体内研究
(In Vivo)

Torin 2 (Torin2) 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[1]. Torin 2 (Torin2) 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[2]. Treatment with Torin 2 (Torin2) 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[3].

分子量

432.40

性状

Solid

Formula

C24H15F3N4O

CAS 号

1223001-51-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 15.62 mg/mL(36.12 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.3127 mL11.5634 mL23.1267 mL
5 mM0.4625 mL2.3127 mL4.6253 mL
10 mM0.2313 mL1.1563 mL2.3127 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% 1-Methyl-2-pyrrolidinone    90%PEG300

    Solubility: ≥ 2 mg/mL (4.63 mM); Clear solution

  • 2.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 1.56 mg/mL (3.61 mM); Clear solution

    此方案可获得 ≥ 1.56 mg/mL (3.61 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 15.6 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
*以上所有助溶剂都可在本网站选购。