Antibodies
Torin 2
- 貨號 Cat. No.
- S2817
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
Torin 2
Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM, respectively.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM, respectively. | |||||
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| Targets | mTOR | ATM | ATR | DNA-PK | ||
| IC50 | 0.25 nM [1] | 28 nM | 35 nM | 118 nM [5] | ||
| In vitro | Torin 2 has the same binding mode as PI3Kγ, V882 serves as a hinge binding point and in the inner hydrophobic pocket Y867, D841 and D964 provide three more hydrogen bonds with aminopyridine side chain analogous to Y2225, D2195 and D2357 of mTOR. [1] Torin 2 inhibits mTORC1, thus activates TFEB by promoting its nuclear translocation with EC50 of 1.666 mM. [2] Torin 2(< 50 nM) causes a significant reduction in viability of both MZ-CRC-1 and TT cells. Torin 2 (100 nM) exerts a significant reduction of migration of both MZ-CRC-1 and TT cells. [3] | |||||
| In vivo | Torin 2 exhibits >95% pharmacodynamic response and half-time of 11.7 min in the mouse liver microsome stability study. Torin 2 exhibits the best bioavailability (51%), short half-life (0.72 hours) and low clearance(19.6 mL/min/kg) in male Swiss albino mice following intravenous and oral administration. [1] Torin 2(20mg/kg) ablates MYCN tumors with reduction in MYCN protein levels and induction of apoptosis in Th-MYCN mice. [4] | |||||
| Features | ||||||
Protocol(Only for Reference)
Kinase Assay: [1]
| mTOR and PI3K Cellular Assays | Cellular IC50 values for mTOR are determined using p53−/− MEFs. Cells are treated with vehicle or increasing concentrations of Torin 2 for 1 h and then lyse. Phosphorylation of S6K1 Thr-389 is monitored by immunoblotting using a phospho-specific antibody. Meanwhile, cellular IC50 values for PI3Ka are determined based on phosphorylation of Akt Thr-308 in p53−/−/mLST8−/− MEFs or human PC3 cells expressing the S473D mutant of Akt1. |
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Cell Assay: [3]
| Cell lines | MZ-CRC-1 and TT cells |
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| Concentrations | 50 nM |
| Incubation Time | 3 days or 5 days |
| Method | For viability, MZ-CRC-1 and TT cells are seeded in quadruplicate in 96-well plates (1.0×104 cells per well) in culture media with 2.5% and 4% FBS, respectively. After 24 hours, cells are treated with Torin 2. At the indicated time point, cells are incubated for 3 hours with 10 μL of CellTiter96 AQueous One solution in 100 μL of culture media and absorbance is measured at 490 nm. |
Animal Study: [1]
| Animal Models | male Swiss albino mice |
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| Dosages | 25 mg/kg |
| Administration | Intravenous or oral |
| Solubility | 30% PEG400/0.5% Tween80/5% propylene glycol, 30 mg/mL |
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01233063 | Recruiting | Cardiovascular Disease|Diabetes|Obesity|Aging | Berkeley Analytics, Inc. | 2010-10 |
Chemical Information
| Molecular Weight (MW) | 432.4 |
|---|---|
| Formula | C24H15F3N4O |
| CAS No. | 1223001-51-1 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 20 mg/mL (46 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| In vivo | 30% PEG400/0.5% Tween80/5% propylene glycol, | 30 mg/mL | |
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | Benzo[h]-1,6-naphthyridin-2(1H)-one, 9-(6-amino-3-pyridinyl)-1-[3-(trifluoromethyl)phenyl]- |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.4324 | 4.324 | 8.648 | 12.972 |
Customer Reviews (1)
 Click to enlarge | Rating | |
| Source | Torin 2 purchased from Selleck | |
| Method | ELISA | |
| Cell Lines | Bone marrow derived macrophages | |
| Concentrations | 10 nM | |
| Incubation Time | 1 h | |
| Results |
Product Citations (1)
MNK1 pathway activity maintains protein synthesis in rapalog-treated gliomas. [Grzmil M, et al. J Clin Invest. 2013;10.1172/JCI70198]
PubMed: 24401275
