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Formula | C24H15F3N4O |
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Molecular Weight | 432.4 | CAS No. | 1223001-51-1 | ||||
Solubility (25°C)* | In vitro | DMSO | 30 mg/mL (69.38 mM) | ||||
Water | Insoluble | ||||||
Ethanol | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
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* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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. Torin 2 decreases cell viability and induces autophagy and apoptosis. | ||||||||
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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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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] |
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Data from [Data independently produced by FEBS J, 2014, 281(16), 3591-608]
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Data from [Data independently produced by , , Arterioscler Thromb Vasc Biol, 2018, doi:10.1161/ATVBAHA.118.311321]
Data from [Data independently produced by , , Oncotarget, 2016, 7(48):79842-79853]
Androgen receptor monomers and dimers regulate opposing biological processes in prostate cancer cells [ Nat Commun, 2024, 15(1):7675] | PubMed: 39227594 |
Endothelial Mechanistic Target of Rapamycin Activation with Different Strains of R. rickettsii: Possible Role in Rickettsial Pathogenesis [ Microorganisms, 2024, 12(2)296] | PubMed: 38399700 |
Analysis of ATG4C function in vivo [ Autophagy, 2023, 19(11):2912-2933] | PubMed: 37459465 |
Analysis of ATG4C function in vivo [ Autophagy, 2023, 19(11):2912-2933] | PubMed: 37459465 |
Continuous sensing of nutrients and growth factors by the mTORC1-TFEB axis [ Elife, 2023, 12e74903] | PubMed: 37698461 |
Sequential Treatment with Temozolomide Plus Naturally Derived AT101 as an Alternative Therapeutic Strategy: Insights into Chemoresistance Mechanisms of Surviving Glioblastoma Cells [ Int J Mol Sci, 2023, 24(10)9075] | PubMed: 37240419 |
Myc controls NK cell development, IL-15-driven expansion, and translational machinery [ Life Sci Alliance, 2023, 6(7)e202302069] | PubMed: 37105715 |
Dephosphorylation of 4EBP1/2 Induces Prenatal Neural Stem Cell Quiescence [ bioRxiv, 2023, 2023.02.14.528513] | PubMed: 36824760 |
Characterization of the autophagy-modulating natural compound prodigiosin for the elimination of therapy-resistant tumor cells [ DNB, 2023, ] | PubMed: none |
Pyruvate Facilitates FACT-Mediated γH2AX Loading to Chromatin and Promotes the Radiation Resistance of Glioblastoma [ Adv Sci (Weinh), 2022, 10.1002/advs.202104055] | PubMed: 35048565 |
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