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Torin 1
| Product Name | Torin 1 |
| Price: | Inquiry |
| Catalog No.: | CN00467 |
| CAS No.: | 1222998-36-8 |
| Molecular Formula: | C35H28F3N5O2 |
| Molecular Weight: | 607.62 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | CCC(=O)N1CCN(CC1)c1ccc(cc1C(F)(F)F)n1c(=O)ccc2c1c1cc(ccc1nc2)c1cnc2c(c1)cccc2 |
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| Description | Torin 1 is a potent inhibitor of mTOR with an IC50 of 3 nM. Torin 1 inhibits both mTORC1/2 complexes with IC50 values between 2 and 10 nM. |
| Target | mTORC1:2-10 nM (IC50) mTORC2:2-10 nM (IC50) mTOR:3 nM (IC50) DNA-PK:1 μM (IC50) PI3K-α:1.8 μM (IC50) ATM:0.6 μM (IC50) hVps34:3 μM (IC50) Autophagy |
| In Vitro | Torin1 (250 nM) completely inhibits proliferation and causes a G1/S cell cycle arrest, and decreases cell size to a greater degree than 50 nM rapamycin in wild-type MEFs[1]. Torin1 has more than 800-fold selectivity between mTOR and PI3Kis, and is very selective relative to other PIKK family kinases with the exception of DNA-PK[2]. |
| In Vivo | Torin1 (20 mg/kg, i.p.) is efficacious in a U87MG xenograft model, and demonstrates good pharmacodynamic inhibition of downstream effectors of mTOR in tumor and peripheral tissues[2]. |
| Cell Assay | On Day 0, 96-well plates are seeded with 500 cells per well and grown overnight. On Day 1, cells are treated with the appropriate compounds and subsequently analyzed on Days 3-5. For analysis, plates are incubated for 60 min at room temperature; 50 μL of CellTiter-Glo reagent is added to each well, and plates are mixed on an orbital shaker for 12 min. Luminescence is quantified on a standard plate luminometer. |
| Animal Admin | For pharmacodynamic experiments, torin 1 powder is first dissolved at 25 mg/mL in 100% N-methyl-2-pyrrolidone and then diluted 1:4 with sterile 50% PEG400 prior to injection. Six-week old male C57BL/6 mice are fasted overnight prior to drug treatment. The mice are treated with vehicle (for 10 hr) or 26 (20 mg/kg for 2, 6 or 10 hr) by IP injection, and then refed 1 h prior to sacrifice (CO2 asphyxiation). Tissues 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. |
| Density | 1.4±0.1 g/cm3 |
| Boiling Point | 817.2±65.0 °C at 760 mmHg |
| Flash Point | 448.0±34.3 °C |
| Exact Mass | 607.219482 |
| PSA | 71.33000 |
| LogP | 5.26 |
| Vapour Pressure | 0.0±2.9 mmHg at 25°C |
| Storage condition | -20℃ |