Torin 2

Name: Torin 2
Brand: Selleck Chemicals
SKU: S2817
Rating: 5 (23 reviews)

For research use only. Not for use in humans.

Catalog No.S2817

23 publications

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.

Selleck's Torin 2 has been cited by 23 publications

Cell Metab, 2019, 29(5):1166-1181

PubMed: 30799286 ( click the link to review the publication )

Nature, 2016, 532(7599):389-93

PubMed: 27064903 ( click the link to review the publication )

Nat Commun, 2020, 11(1):71

PubMed: 31900415 ( click the link to review the publication )

Nat Commun, 2019, 10(1):1444

PubMed: 30926899 ( click the link to review the publication )

Nat Commun, 2019, 10(1):1515

PubMed: 30944303 ( click the link to review the publication )

Biomol Ther, 2019, 27(1):34-40

PubMed: 30231606 ( click the link to review the publication )

Mol Cell, 2018, 69(1):100-112

PubMed: 29290610 ( click the link to review the publication )

Nat Commun, 2018, 9(1):2292

PubMed: 29895827 ( click the link to review the publication )

Autophagy, 2018, 14(5):743-763

PubMed: 29173006 ( click the link to review the publication )

Elife, 2018, 7

PubMed: 29595474 ( click the link to review the publication )

Arterioscler Thromb Vasc Biol, 2018, 10.1161/ATVBAHA.118.311321

PubMed: 30026269 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(2):347-354

PubMed: 28958992 ( click the link to review the publication )

Mol Biol Cell, 2018, 29(1):42-52

PubMed: 29118074 ( click the link to review the publication )

Int J Mol Sci, 2018, 19(5)

PubMed: 29757257 ( click the link to review the publication )

Elife, 2017, 6

PubMed: 29239720 ( click the link to review the publication )

Cellular Signalling, 2016, S0898-6568(16)30062-6

PubMed: 27010498 ( click the link to review the publication )

Oncotarget, 2016, 7(48):79842-79853

PubMed: 27821800 ( click the link to review the publication )

Oncotarget, 2016, 7(34):55690-55703

PubMed: 27494886 ( click the link to review the publication )

Cell Rep, 2015, 11(3):446-59

PubMed: 25865887 ( click the link to review the publication )

Oncol Rep, 2015, 34(4):1708-16

PubMed: 26239364 ( click the link to review the publication )

FEBS J, 2014, 281(16):3591-608

PubMed: 24938479 ( click the link to review the publication )

Oncotarget, 2014, 5(20):10034-47

PubMed: 25296981 ( click the link to review the publication )

J Clin Invest, 2013, 124(2):742-54

PubMed: 24401275 ( click the link to review the publication )

Purity & Quality Control

Choose Selective mTOR Inhibitors

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	M1zaeGZ2dmO2aX;uJIF{e2G7				NF\z[W9KdmirYnn0bY9vKG:oIGDJN2tidHCqYTDpckBpfW2jbjDQR\|Mh[2WubIOg[ZhxemW\|c3nu[{BCc3RzIGO0O\|NFKG23dHHueEBie3Onc4Pl[EBieyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0JHRpejNyODDifUBqdW23bn;icI91fGmwZzygSWM2OD1yLkKg{txO	M1fYTVIyOzJ{NU[2

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-S6K / S6K / p-AKT / AKT / IRS1 / p-4EBP1 / 4EBP1 / p-GSK3; PubMed: 23436801 Cancer Res Torin2 is a potent mTOR inhibitor in HCT-116 cells p-Chk1 / Chk1 / p-Chk2 / Chk2 / p-DNA-PK ; PubMed: 23436801 Cancer Res Torin2 inhibits ATR (UV radiation), ATM and DNA-PK (ionizing radiation) strongly.	23436801
Immunofluorescence	LC3B ; PubMed: 23436801 Cancer Res Hela cells were treated with indicated concentrations of Torin2 for 3 days stained with antibody specific for LC3B and DAPI.	23436801
Growth inhibition assay	Cell viability; PubMed: 24434750 Sci Rep Concentration–response curves of Torin 2, Torin 1 and WWH030 against gametocytes measured in the high throughout viability assay. Torin 1 was much weaker in potency compared to Torin 2.	24434750

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]	- Collapse 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]	- Collapse 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]	- Collapse 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

- Collapse

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
Smiles	NC1=CC=C(C=N1)C2=CC=C3N=CC4=C(N(C(=O)C=C4)C5=CC=CC(=C5)C(F)(F)F)C3=C2

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mTOR Signaling Pathway Map

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Most Potent mTOR Inhibitor

Rapamycin (Sirolimus) : mTOR, IC50=~0.1 nM.
FDA-approved mTOR Inhibitor

Temsirolimus (CCI-779, NSC 683864) : Approved by FDA for Renal Cell Carcinoma (RCC).
Newest mTOR Inhibitor

XL388 ^New : Highly potent, selective, ATP-competitive inhibitor of mTOR with IC50 of 9.9 nM, 1000-fold selectivity over the closely related PI3K kinases.

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Dorsomorphin (Compound C) ^New

Dorsomorphin is a potent, reversible, selective AMPK inhibitor with K_i of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type I BMP receptor activity.
Rapamycin (Sirolimus)

Rapamycin (Sirolimus) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells.
Everolimus (RAD001)

Everolimus (RAD001) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay.
AZD8055

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Features:First drug to inhibit both types of mTOR protein.
Torin 1

Torin 1 is a potent inhibitor of mTORC1/2 with IC50 of 2 nM/10 nM in cell-free assays; exhibits 1000-fold selectivity for mTOR than PI3K.
Temsirolimus (CCI-779)

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Sapanisertib (MLN0128)

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Torin 2