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Formula | C35H28F3N5O2 |
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Molecular Weight | 607.62 | CAS No. | 1222998-36-8 | |
Solubility (25°C)* | In vitro | DMSO | 3 mg/mL (4.93 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <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 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. | |||||||||||
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Targets |
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In vitro | Torin1 inhibits phosphorylation of mTORC1 and mTORC2 substrates in cells at concentrations of 2 and 10 nM, respectively. Moreover, Torin1 exhibits 1000-fold selectivity for mTOR over PI3K (EC50 = 1800 nM) and exhibits 100-fold binding selectivity relative to 450 other protein kinases. [1] [2] Torin1 causes cell cycle arrest through a rapamycin-resistant mechanism that is also independent of mTORC2. Torin1 disrupts mTORC1-dependent phenotypes more completely than rapamycin. Rapamycin-resistant functions of mTORC1 are required for cap-dependent translation. [1] In a recent study, it is reported Torin1 increases neurotensin secretion and gene expression through activation of the MEK/ERK/c-Jun pathway in the human endocrine cell line BON. [3] | |||||||||||
In vivo | Torin1 is efficacious at a dose of 20 mg/kg in a U87MG xenograft model and demonstrates good pharmacodynamic inhibition of downstream effectors of mTOR in tumor and peripheral tissues. [2] |
Kinase Assay:[1] |
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Cell Assay:[1] |
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Animal Study:[2] |
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Data from [Data independently produced by Am J Pathol, 2014, 184(1), 214-29]
Data from [Data independently produced by Mol Cell Biol, 2014, 34(24), 4474-84]
Data from [Data independently produced by Biochem Biophys Res Commun, 2014, 10.1016/j.bbrc.2014.05.047]
Data independently produced by , , Lim Hsiu Kim, Lina from National University of Singapore
Akt enhances the vulnerability of cancer cells to VCP/p97 inhibition-mediated paraptosis [ Cell Death Dis, 2024, 15(1):48] | PubMed: 38218922 |
MTOR Suppresses Cigarette Smoke-Induced Airway Inflammation and MMP12 Expression in Macrophage in Chronic Obstructive Pulmonary Disease [ Int J Chron Obstruct Pulmon Dis, 2024, 19:269-279] | PubMed: 38288346 |
Lysosomes mediate the mitochondrial UPR via mTORC1-dependent ATF4 phosphorylation [ Cell Discov, 2023, 9(1):92] | PubMed: 37679337 |
Lysosomes mediate the mitochondrial UPR via mTORC1-dependent ATF4 phosphorylation [ Cell Discov, 2023, 9(1):92] | PubMed: 37679337 |
PD-1 instructs a tumor-suppressive metabolic program that restricts glycolysis and restrains AP-1 activity in T cell lymphoma [ Nat Cancer, 2023, 4(10):1508-1525] | PubMed: 37723306 |
Analysis of ATG4C function in vivo [ Autophagy, 2023, 19(11):2912-2933] | PubMed: 37459465 |
Direct regulation of FNIP1 and FNIP2 by MEF2 sustains MTORC1 activation and tumor progression in pancreatic cancer [ Autophagy, 2023, 1-20.] | PubMed: 37772772 |
Analysis of ATG4C function in vivo [ Autophagy, 2023, 19(11):2912-2933] | PubMed: 37459465 |
SARS-CoV-2 ORF7a blocked autophagy flux by intervening in the fusion between autophagosome and lysosome to promote viral infection and pathogenesis [ J Med Virol, 2023, 10.1002/jmv.29200] | PubMed: 37916857 |
NCoR1 controls Mycobacterium tuberculosis growth in myeloid cells by regulating the AMPK-mTOR-TFEB axis [ PLoS Biol, 2023, 21(8):e3002231] | PubMed: 37590294 |
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