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

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.

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/P_i 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

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	MYPGeY5kfGmxbjDhd5NigQ>?				M{ntS2lvcGmkaYTpc44hd2ZiUFmzT4FteGijIHnuJIh2dWGwIGDDN{Bk\WyuczDlfJBz\XO\|aX7nJGFsfDFiU{S3N2QhdXW2YX70JIF{e2W\|c3XkJIF{KHCqb4PwbI9zgWyjdHnvckBw\iCDa4SgWIhzOzB6IHL5JIludXWwb3Lsc5R1cW6pLDDFR\|UxRTBwMjFOwG0>	MXGyNVMzOjV4Nh?=

... 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]	+ Expand 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]	+ Expand 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)

References

+ Expand

Solubility (25°C)

In vitro	DMSO	20 mg/mL (46.25 mM)
	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 Download Torin 2 SDF

Molecular Weight	432.4
Formula	C₂₄H₁₅F₃N₄O
CAS No.	1223001-51-1
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A

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Torin 2