Torin 2
Catalog No.S2817
Molecular Weight(MW): 432.4
Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53−/− MEFs cell line; 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,in PC3 cell lines respectively.
4 Customer Reviews
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U2OS cells were plated in six-well plates using complete medium. The next day the cells were washed four times with NaCl/Pi before maintaining them for 6 h in serum- and glucose-free DMEM supplemented as indicated in the absence or presence of 0.1 uM Torin 2 for the last 1 h. The cells were control- treated, treated with 1 ug/mL insulin or treated with 1 mM H2O2 for 15 min. Thereafter, cell lysates were prepared and western blotting was performed using the indicated antibodies.
FEBS J 2014 281(16), 3591-608. Torin 2 purchased from Selleck.
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Bone marrow derived macrophages were pre-treated with 10nM Torin for 1h prior to LPS treatment (100 ng/ml). TNF-a production was analyzed 24h later.
Torin 2 purchased from Selleck.
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Immunofluorescent imaging of HAECs using VE-CAD (red) and p120 (green) antibodies was performed 12 h after DMSO (control), Torin-2 (100 nM), or EVL (500 nM) treatments. White arrows denote interendothelial gaps. White bar indicates 50 μm. EVL treatment increased VE-CAD mobilization from the membrane into the cytosol (relative to DMSO) with evidence of intracellular deposits and interendothelial gaps, whereas in DMSO-treated cells, there was colocalization of p120 and VE-CAD (yellow border) with no evidence of gap formation. In Torin-2-treated cells, there was evidence of colocalization of p120 and VE-CAD at cell borders with minimal interendothelial gap formation.
Arterioscler Thromb Vasc Biol, 2018, doi:10.1161/ATVBAHA.118.311321. Torin 2 purchased from Selleck.
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A. Western Blot analysis in the ALL-SIL cell line treated with single administration of Imatinib, Nilotinib, GZD824, Torin-2 and BGT226 for 24 h. An increase of expression of fast-migrating (lipidated) LC3A/B after drug treatments is shown. Twenty-five μg of protein were blotted on each lane. β-Actin documented equal lane loading. B. Flow cytometric analysis of autophagy in the ALL-SIL and PEER cell lines treated with single or combined administration of Imatinib, Nilotinib, GZD824 with Torin-2 or BGT226 for 24 h. CTRL, control (untreated) cells. Asterisks indicate significant differences in comparison to single drug treated samples (*p< 0.05). Imatinib, Nilotinib, GZD824, Torin-2 and BGT226 were abbreviated in IMA, NIL, GZD, TOR and BGT.
Oncotarget, 2016, 7(48):79842-79853. Torin 2 purchased from Selleck.
Purity & Quality Control
Choose Selective mTOR Inhibitors
Biological Activity
| Description | Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53−/− MEFs cell line; 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,in PC3 cell lines respectively. | ||||||||||||||||
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| Targets |
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| 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] |
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| Cell Data |
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| Assay |
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| 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] |
Protocol
| Kinase Assay:[1] |
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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 Research:[3] |
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| Animal Research:[1] |
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Solubility (25°C)
| In vitro | DMSO | 20 mg/mL (46.25 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 30% PEG400+0.5% Tween80+5% propylene glycol For best results, use promptly after mixing. |
30 mg/mL |
* 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 Information
| Molecular Weight | 432.4 |
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| Formula | C24H15F3N4O |
| CAS No. | 1223001-51-1 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
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