1-[4-[4-(1-Oxopropyl)-1-piperazinyl]-3-(trifluoromethyl)phenyl]-9-(3-quinolinyl)benzo[h]-1,6-naphthyridin-2(1H)-one
1-[4-[4-(1-Oxopropyl)-1-piperazinyl]-3-(trifluoromethyl)phenyl]-9-(3-quinolinyl)benzo[h]-1,6-naphthyridin-2(1H)-one
CAS: 1222998-36-8
Molecular Formula: C35H28F3N5O2
1-[4-[4-(1-Oxopropyl)-1-piperazinyl]-3-(trifluoromethyl)phenyl]-9-(3-quinolinyl)benzo[h]-1,6-naphthyridin-2(1H)-one - Names and Identifiers
1-[4-[4-(1-Oxopropyl)-1-piperazinyl]-3-(trifluoromethyl)phenyl]-9-(3-quinolinyl)benzo[h]-1,6-naphthyridin-2(1H)-one - Physico-chemical Properties
| Molecular Formula | C35H28F3N5O2 |
| Molar Mass | 607.62 |
| Density | 1.362 |
| Melting Point | >223°C (dec.) |
| Boling Point | 817.2±65.0 °C(Predicted) |
| Solubility | Soluble in DMSO (up to 8 mg/ml). |
| Appearance | Yellowish-white powder |
| Color | White or off-white |
| pKa | 4.19±0.20(Predicted) |
| Storage Condition | +2C to +8C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months. |
| Physical and Chemical Properties | Bioactive Torin 1 is a potent mTORC1/2 inhibitor with an IC50 of 2 nM/10 nM in a cell-free assay; Acting on mTOR is 1000-fold more selective than acting on PI3K. |
| In vitro study | Torin1 inhibits phosphorylation of mTORC1 and mTORC2 substrates in cells at concentrations of 2 and 10 nM, respectively. Moreover, Torin1 exhibits 1000-fold selectivity for mTOR over PI3K (EC50=1800 nM) and exhibits 100-fold binding selectivity relative to 450 other protein kinases. Torin1 causes cell cycle arrest through a rapamycin-resistant mechanism that is also independent of mTORC2. Torin1 disrupts mTORC1-dependent phenotypes more completely than rapamycin. Rapamycin-resistant functions of mTORC1 are required for cap-dependent translation. In a recent study, it is reported Torin1 increment neurotensin secret and gene expression through activation of the MEK/ERK/c-Jun pathway in the human endocrine cell line BON. Torin1 inhibits phosphorylation of mTORC1 and mTORC2 substrates at 2 and 10 nM concentrations, respectively. In addition, Torin1 was 1800-fold more selective for mTOR than PI3K (EC50=1000 nM) and 450-fold more selective for binding to 100 other protein kinases. Torin1 causes cell cycle arrest by a rapid resistant mechanism, and it is independent of mTORC2. Torin1 interferes with the mtorc1-dependent phenotype more completely than does rapamylin. Cap-dependent translation requires the ability of mTORC1 to be resistant to Rapamycin. In a recent study, Torin1 was reported to activate the human endocrine cell line BON MEK/ERK/c-Jun pathway can increase neurotensin secretion and gene expression. |
| In vivo study | Torin1 is effective at a dose of 20 mg/kg. Torin1 was effective in the U87MG xenograft model at a dose of 20 mg/kg and showed good pharmacodynamic inhibition of mTOR downstream effector proteins in tumor and peripheral tissues. |
1-[4-[4-(1-Oxopropyl)-1-piperazinyl]-3-(trifluoromethyl)phenyl]-9-(3-quinolinyl)benzo[h]-1,6-naphthyridin-2(1H)-one - Risk and Safety
| Safety Description | 24/25 - Avoid contact with skin and eyes. |
| HS Code | 29334900 |
1-[4-[4-(1-Oxopropyl)-1-piperazinyl]-3-(trifluoromethyl)phenyl]-9-(3-quinolinyl)benzo[h]-1,6-naphthyridin-2(1H)-one - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.646 ml | 8.229 ml | 16.458 ml |
| 5 mM | 0.329 ml | 1.646 ml | 3.292 ml |
| 10 mM | 0.165 ml | 0.823 ml | 1.646 ml |
| 5 mM | 0.033 ml | 0.165 ml | 0.329 ml |
Last Update：2024-01-02 23:10:35
1-[4-[4-(1-Oxopropyl)-1-piperazinyl]-3-(trifluoromethyl)phenyl]-9-(3-quinolinyl)benzo[h]-1,6-naphthyridin-2(1H)-one - Reference Information
| biological activity | Torin 1 is an effective mTORC1/2 inhibitor with IC50 of 2 nM/10 nM; The selectivity of acting on mTOR is 1000 times higher than that of acting on PI3K. Torin 1 is an effective mTORC1/2 inhibitor. IC50 is 2 nM/10 nM in cell-free test. The selectivity of mTOR is 1000 times higher than that of PI3K. |
| in vitro studies | Torin1 inhibits phosphorylation of mTORC1 and mTORC2 substrates in cells at concentrations of 2 and 10 nM, respectively. Moreover, torin1 exhibits 1000-fold selectivity for mTOR over PI3K (EC50=1800 nM) and exhibits 100-fold binding selectivity relative to 450 other protein kinases. Torin1 problems cell through a rapamycin-resistant mechanism that is also independent of mTORC2. Torin1 disrupts mTORC1-dependent phenotypes more completely than rapamycin. Rapamycin-resistant functions of mTORC1 are required for cap-dependent translation. In a real study, it is reported Torin1 increases neurotensin secretion and gene expression through activation of the MEK/ERK/c-Jun pathway in the human endocrine cell line BON. Torin1 inhibited the phosphorylation of mTORC1 and mTORC2 substrates at 2 and 10 nM concentrations, respectively. In addition, Torin1 is 1000 times more selective for mTOR than PI3K (EC50=1800 nM) and 100 times more selective for binding than 450 other protein kinases. Torin1 causes cell cycle arrest through rapamycin resistance mechanisms, and it does not depend on mTORC2. Torin1 interferes with mTORC1 dependent phenotype more completely than rapamycin. Cap-dependent translation requires mTORC1 to be Rapamycin resistant. In a recent study, it has been reported that Torin1 can increase neurotensin secretion and gene expression by activating MEK/ERK/c-Jun pathway in human endocrine cell line BON. |
| in vivo study | Torin1 is efficacious at a dose of 20 mg/kg in a U87MG xenograft model and demonstrates good pharmacodynamic inhibition of downstream effectors of mTOR in tumor and peripheral tissues. Torin1 at a dose of 20 mg/kg, it is effective in the U87MG xenograft model and shows good pharmacodynamic inhibition of mTOR downstream effector proteins in tumor and peripheral tissues. |
| target | TargetValue mTORC1 (Cell-Free Assay) 2 nM MTOR (Cell-Free Assay) 4.32 nM DNA-PK (Cell-Free Assay) 6.34 nM mTORC2 (Cell-Free Assay) 10 nM p110γ (Cell-Free Assay) 171 nM |
| Target | Value |
| mTORC1 (Cell-free assay) | 2 nM |
| mTOR (Cell-free assay) | 4.32 nM |
| DNA-PK (Cell-free assay) | 6.34 nM |
| mTORC2 (Cell-free assay) | 10 nM |
| p110γ (Cell-free assay) | 171 nM |
Last Update：2024-04-10 22:29:15
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Product Name: Torin 1 Visit Supplier Webpage Request for quotationCAS: 1222998-36-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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