1. PI3K/Akt/mTOR
    Autophagy
  2. mTOR
    Autophagy

Torin 2 

Cat. No.: HY-13002 Purity: 99.89%
Data Sheet SDS Handling Instructions

Torin 2 is an mTOR inhibitor with EC50 of 0.25 nM, and exhibits 800-fold selectivity over PI3K (EC50: 200 nM).

For research use only. We do not sell to patients.
Torin 2 Chemical Structure

Torin 2 Chemical Structure

CAS No. : 1223001-51-1

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10 mM * 1 mL in DMSO $88 In-stock
5 mg $80 In-stock
10 mg $110 In-stock
50 mg $330 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Torin 2 is an mTOR inhibitor with EC50 of 0.25 nM, and exhibits 800-fold selectivity over PI3K (EC50: 200 nM).

IC50 & Target

EC50: 0.25 nM (mTOR), 200 nM (PI3K)[1]

In Vitro

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[1]. 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[2].

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].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.3127 mL 11.5634 mL 23.1267 mL
5 mM 0.4625 mL 2.3127 mL 4.6253 mL
10 mM 0.2313 mL 1.1563 mL 2.3127 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[2]

Torin 2 (Torin2) is dissolved in DMSO and stored, and then diluted with appropriate media before use[2].

HCT116 cells are treated with 100 nM Torin 2 or AZD8055 for 1 hour before they are thoroughly washed out by 3×PBS and 1×DMEM medium. Then cells are incubated in DMEM medium for indicated time before they are lysed and collected using M-PER. Protein concentrations are measured and equal amount of proteins are loaded. Experiments are repeated three times and one set of results[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1][3]

Torin 2 (Torin2) is dissolved at 25 mg/mL in 100% N-methyl-2-pyrrolidone and then diluted 1:4 with sterile 50% PEG400 prior to injection (Mice)[1].

Mice[1]
Six-week old male C57BL/6 mice are fasted overnight prior to Torin 2 treatment. The mice are treated with vehicle (for 10 h) or Torin 2 (20 mg/kg for 6h) via oral gavage and then re-fed 1 h prior to sacrifice (CO2 asphyxiation). Liver and lung are collected and frozen on dry ice. The frozen tissue is thawed on ice and lysed by sonication in tissue lysis buffer (50 mM HEPES, pH 7.4, 40 mM NaCl, 2 mM EDTA, 1.5 mM sodium orthovanadate, 50 mM sodium fluoride, 10 mM sodium pyrophosphate, 10 mM sodium β-glycerophosphate, 0.1% SDS, 1.0% sodium deoxycholate, and 1.0% Triton, supplemented with protease inhibitor cocktail tablets). The concentration of clear lysate is measured using the Bradford assay and samples are subsequently normalized by protein content and analyzed by SDS-PAGE and immunoblotting.
Rat[3]
Female rats (220 g) are group-housed 4 animals per cage, and kept on a 12-hour light/dark cycle with food and water ad libitum. Spinal cord injury is done with the Keck Center for Neurosciences impactor using a 10 g weight dropped from a height of 25 mm onto the dorsal surface of the exposed spinal cord. After recording BBB scores, withdrawal thresholds evoked by touch stimulus, and body weights for the first week post-injury, animals are divided into 5 treatment groups: naïve (N=4), sham (N=6), vehicle (N=6), Torin 2 (N=6), and Torin 2+Rapamycin (N=8). Torin 2 alone (4 mg/kg) or in combination with Rapamycin (1.5 mg/kg) is administered orally by gavage once a day starting at day 15 after injury and ending at day 29. In sham operated rats only the laminectomy is performed. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

432.4

Formula

C₂₄H₁₅F₃N₄O

CAS No.

1223001-51-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Torin 2
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