Torin 2 |
Catalog No.GC13858
One-Click Copy Product Info
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Torin 2 is an orally active mTOR inhibitor (EC50=0.25nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1223001-51-1
Sample solution is provided at 25 µL, 10mM.
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Torin 2 is an orally active mTOR inhibitor (EC50=0.25nM). Torin 2 inhibits mTORC1/2-mediated phosphorylation of S6K and 4EBP1 to block protein synthesis and cell proliferation. Torin 2 enhances DNA damage response and radiotherapy sensitivity by inhibiting ATM, ATR, and DNA-PK. Torin 2 can be used for research on tumors, autophagy, and DNA damage repair[1-4].
In vitro, treatment of Kelly, IMR-32, and SK-N-BE(2) cells with 11.69-29.67nM Torin 2 for 72 hours inhibited cell viability and induced G1 cell cycle arrest[5]. Treatment of NALM-6, SEM, REH, RS4;11, BV-173, SUP-B15, TOM-1, and B-precursor ALL cells with 0.025-0.5μM Torin 2 for 48 hours inhibited cell proliferation, arrested cells in G0/G1 phase, and reduced S phase cell proportion[6]. Treatment of HepG2 cells with 46μM Torin 2 for 72 hours produced cytotoxicity[7].
In vivo, daily oral gavage of 40mg/kg Torin 2 for 2 days to Lox-Stop-Lox-Kras(G12D) mice after intranasal Ad-Cre induction of Kras G12D expression inhibited pS6K, p4EBP1, and pAkt expression in tumor tissues[8]. Single oral gavage of 20mg/kg Torin 2 to fasted C57BL/6 mice overnight maintained strong inhibition of mTOR activity and reduced S6K T389 and Akt T308 phosphorylation in lung and liver tissues for at least 6 hours[9].
References:[1] Vershinina YS, Krasnov GS, Garbuz DG, et al. Transcriptomic Analysis of the Effect of Torin-2 on the Central Nervous System of Drosophila melanogaster. Int J Mol Sci. 2023 May 22;24(10):9095.
[2] Krishnan K, Ziniel P, Li H, et al. Torin 2 Derivative, NCATS-SM3710, Has Potent Multistage Antimalarial Activity through Inhibition of P. falciparum Phosphatidylinositol 4-Kinase (Pf PI4KIIIβ). ACS Pharmacol Transl Sci. 2020 Sep 11;3(5):948-964.
[3] Waetzig R, Matthes M, Leister J, et al. Comparing mTOR inhibitor Rapamycin with Torin-2 within the RIST molecular-targeted regimen in neuroblastoma cells. Int J Med Sci. 2021 Jan 1;18(1):137-149.
[4] Maddineni P, Kaipa BR, Kodati B, et al. Pharmacological restoration of impaired autophagy in retinal ganglion cells prevents abnormal mitochondrial accumulation and glaucomatous neurodegeneration. Mol Neurodegener. 2026;21:30.
[5] Waetzig R, Matthes M, Leister J, et al. Comparing mTOR inhibitor Rapamycin with Torin-2 within the RIST molecular-targeted regimen in neuroblastoma cells. Int J Med Sci. 2021;18(1):137-149.
[6] Simioni C, Cani A, Martelli AM, et al. Activity of the novel mTOR inhibitor Torin-2 in B-precursor acute lymphoblastic leukemia and its therapeutic potential to prevent Akt reactivation. Oncotarget. 2014;5(20):10034-10047.
[7] Sun W, Tanaka TQ, Magle CT, et al. Chemical signatures and new drug targets for gametocytocidal drug development. Sci Rep. 2014 Jan 17;4:3743.
[8] Liu Q, Xu C, Kirubakaran S, et al. Characterization of Torin2, an ATP-competitive inhibitor of mTOR, ATM and ATR. Cancer Res. 2013 Apr 15;73(8):2574-2586.
[9] Liu Q, Wang J, Kang SA, 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 mTOR inhibitor for treatment of cancer. J Med Chem. 2011 Mar 10;54(5):1473-1480.
| Cell experiment [1]: | |
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Cell lines |
Kelly cells (human neuroblastoma cell line), IMR-32 cells (human neuroblastoma cell line), SK-N-BE(2) cells (human neuroblastoma cell line) |
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Preparation Method |
Kelly, IMR-32 and SK-N-BE(2) cells were maintained in RPMI 1640 or EMEM/Ham's F12 medium supplemented with FBS at 37°C, 5% CO2. Cells were treated with Torin 2 at concentrations of 11.69nM, 29.67nM and 28.52nM respectively for 72 hours. After treatment, cell viability was measured by MTT assay, cell cycle distribution was analyzed by propidium iodide staining, and protein expression was analyzed by immunoblot. |
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Reaction Conditions |
11.69nM-29.67nM; 72h |
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Applications |
Torin 2 inhibited cell viability in Kelly, IMR-32 and SK-N-BE(2) cells. Torin 2 induced G1 cell cycle arrest in Kelly and IMR-32 cells. Torin 2 marginally induced PARP-1 cleavage at 160nM in Kelly and IMR-32 cells. Torin 2 did not increase LC3B-II expression at IC50 concentrations in Kelly and IMR-32 cells. |
| Animal experiment [2]: | |
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Animal models |
Lox-Stop-Lox-Kras(G12D) mice |
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Preparation Method |
Mice were given Ad-Cre by nasal inhalation at 5-7 weeks of age to induce Kras G12D expression. After initial imaging, mice bearing tumor were given Torin 2 (40mg/kg) or Torin 2 (40mg/kg) combined with AZD6244 (25mg/kg) by oral gavage daily. For pharmacodynamics assay, mice were treated with a single daily dosing of Torin 2 (40mg/kg) for 2 days and sacrificed for immunohistochemical analyses. |
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Dosage form |
40mg/kg; p.o.; daily for 2 days |
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Applications |
Torin 2 strongly suppressed pS6K(T389) and p4EBP1(T37/46) and partly suppressed pAkt(T308) in tumor tissues. Torin 2 combined with AZD6244 for 4 weeks significantly reduced tumor volume and reduced tumor FDG metabolic activity. |
| References: [1] Waetzig R, Matthes M, Leister J, et al. Comparing mTOR inhibitor Rapamycin with Torin-2 within the RIST molecular-targeted regimen in neuroblastoma cells. Int J Med Sci. 2021;18(1):137-149. [2] Liu Q, Xu C, Kirubakaran S, et al. Characterization of Torin2, an ATP-competitive inhibitor of mTOR, ATM and ATR. Cancer Res. 2013 Apr 15;73(8):2574-2586. | |
| Cas No. | 1223001-51-1 | SDF | |
| Chemical Name | 9-(6-aminopyridin-3-yl)-1-[3-(trifluoromethyl)phenyl]benzo[h][1,6]naphthyridin-2-one | ||
| Canonical SMILES | C1=CC(=CC(=C1)N2C(=O)C=CC3=CN=C4C=CC(=CC4=C32)C5=CN=C(C=C5)N)C(F)(F)F | ||
| Formula | C24H15F3N4O | M.Wt | 432.41 |
| Solubility | ≥ 21.6mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3126 mL | 11.5631 mL | 23.1262 mL |
| 5 mM | 462.5 μL | 2.3126 mL | 4.6252 mL |
| 10 mM | 231.3 μL | 1.1563 mL | 2.3126 mL |
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g
μL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)