Torin 2

Catalog No.S2817

Torin 2 Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 190 In stock
USD 110 In stock
USD 170 In stock
USD 370 In stock
USD 570 In stock
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3 Customer Reviews

  • 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.

    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.

  •  

    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.

Purity & Quality Control

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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.
Targets
mTOR [1]
(p53−/− MEFs)
ATM [5]
(PC3 cells)
ATR [5]
(PC3 cells)
DNA-PK [5]
(PC3 cells)
0.25 nM 28 nM(EC50) 35 nM(EC50) 118 nM(EC50)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human PC3 cells NYS2PFJYTnWwY4Tpc44h[XO|YYm= MX3Jcohq[mm2aX;uJI9nKFCLM1vhcJBp[SCrbjDoeY1idiCSQ{OgZ4VtdHNiZYjwdoV{e2mwZzDBb5QyKFN2N{PEJI12fGGwdDDhd5Nme3OnZDDhd{BxcG:|cHjvdplt[XSrb36gc4YhSWu2IGTodlMxQCCkeTDpcY12dm:kbH;0eIlv\yxiRVO1NF0xNjJizszN M1ntcFIyOzJ{NU[2

... Click to View More Cell Line Experimental Data

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.
Cell Research:[3]
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  • Cell lines: MZ-CRC-1 and TT cells
  • 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: male Swiss albino mice
  • Formulation: first dissolve at 25 mg/mL in 100% N-methyl-2-pyrrolidone and then dilute 1:4 with sterile 50% PEG400 prior to injection
  • Dosages: 25 mg/kg
  • Administration: Intravenous or oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 20 mg/mL (46.25 mM)
Water slightly soluble or insoluble
Ethanol slightly soluble or insoluble
In vivo Add solvents individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
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
Formula

C24H15F3N4O

CAS No. 1223001-51-1
Storage powder
in solvent
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID