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Submit ReviewTorin 2 is a potent and selective mTOR inhibitor (IC50 = 2.1 nM). Displays 800-fold cellular selectivity for mTOR over PI3K (cellular EC50 values are 0.25 and 200 nM for mTOR and PI3K respectively). Activates autophagy. Orally available.
Sold under license from Whitehead Institute for Biomedical Research.
Torin 2 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
分子量 | 432.4 |
公式 | C24H15F3N4O |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1223001-51-1 |
PubChem ID | 51358113 |
InChI Key | GUXXEUUYCAYESJ-UHFFFAOYSA-N |
Smiles | O=C(C=C3)N(C5=CC=CC(C(F)(F)F)=C5)C2=C3C=NC1=CC=C(C4=CC=C(N)N=C4)C=C12 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 8.65 | 20 |
以下数据基于产品分子量 432.4。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.2 mM | 11.56 mL | 57.82 mL | 115.63 mL |
1 mM | 2.31 mL | 11.56 mL | 23.13 mL |
2 mM | 1.16 mL | 5.78 mL | 11.56 mL |
10 mM | 0.23 mL | 1.16 mL | 2.31 mL |
参考文献是支持产品生物活性的出版物。
Liu et al (2011) Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer. J.Med.Chem. 54 1473 PMID: 21322566
Simioni et al (2014) Activity of the novel mTOR inhibitor Torin-2 in B-precursor acute lymphoblastic leukemia and its therapeutic potential to prevent Akt reactivation. Oncotarget 30 10034 PMID: 25296981
Galluzzi et al (2017) Pharmacological modulation of autophagy: therapeutic potential and persisting obstacles. Nat.Rev.Drug.Discov. PMID: 28529316
If you know of a relevant reference for Torin 2, please let us know.
关键词: Torin 2, Torin 2 supplier, Torin2, mtor, mammalian, target, rapamycin, selective, inhibitors, inhibits, mTOR, Autophagy, 4248, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Torin 2 的部分引用包括:
Pankaj K et al (2020) The Synergistic Effect of an ATP-Competitive Inhibitor of mTOR and Metformin on Pancreatic Tumor Growth. Curr Dev Nutr 4 nzaa131 PMID: 32908958
Soliman et al (2017) Effects of MET and a Mammalian Target of Rapamycin (mTOR) ATP-Competitive Inhibitor on Targeted Metabolomics in Pancreatic Cancer Cell Line. Metabolomics (Los Angel) 6 PMID: 28217402
Hwang et al (2013) Protein phosphatase 2A isoforms utilizing Aβ scaffolds regulate differentiation through control of Akt protein. J Biol Chem 288 32064 PMID: 24052256
Ginzberg et al (2018) Cell size sensing in animal cells coordinates anabolic growth rates and cell cycle progression to maintain cell size uniformity. Elife 7 PMID: 29889021
Al-Ali et al (2017) The mTOR Substrate S6 Kinase 1 (S6K1) Is a Negative Regulator of Axon Regeneration and a Potential Drug Target for Central Nervous System Injury. J Neurosci 37 7079 PMID: 28626016
Toops et al (2015) Cholesterol-mediated activation of acid sphingomyelinase disrupts autophagy in the retinal pigment epithelium. Nat Commun 26 41640 PMID: 25378587
Yu et al (2015) PI3K/mTORC2 regulates TGF-β/AVNsignalling by modulating Smad2/3 activity via linker phosphorylation. BMC Biochem 6 7212 PMID: 25998442
Han et al (2014) Parallel measurement of dynamic changes in translation rates in single cells. Nat Methods 11 86 PMID: 24213167
Ahmed et al (2014) High prevalence of mTOR complex activity can be targeted using Torin2 in papillary thyroid carcinoma. Carcinogenesis 35 1564 PMID: 24583924
Yan et al (2021) Liquid culture system for efficient depletion of the endogenous nutrients in Arabidopsis seedlings. STAR Protoc 2 100922 PMID: 34761234
Sung Hoon et al (2021) Translation Inhibitors Activate Autophagy Master Regulators TFEB and TFE3. Int J Mol Sci 22 PMID: 34769510
Selim et al (2021) Comparing mTOR inhibitor Rapamycin with Torin-2 within the RIST molecular-targeted regimen in neuroblastoma cells. Int J Med Sci 18 137-149 PMID: 33390782
Markus A et al (2015) Conditional disruption of rictor demonstrates a direct requirement for mTORC2 in skin tumor development and continued growth of established tumors. Carcinogenesis 36 487-97 PMID: 25740823
Hussain et al (2015) Dual Targeting of mTOR Activity with Torin2 Potentiates Anticancer Effects of cisp. in Epithelial Ovarian Cancer. Mol Med 21 466 PMID: 26023849
Montané and Menand (2013) ATP-competitive mTOR kinase inhibitors delay plant growth by triggering early differentiation of meristematic cells but no developmental patterning change. J Virol 64 4361 PMID: 23963679
Lei et al (2017) SYK kinase mediates brown fat differentiation and activation. Nat Commun 8 2115 PMID: 29235464
Jennewein et al (2016) Diagnostic and clinical relevance of the autophago-lysosomal network in human gliomas. Oncotarget 7 20016 PMID: 26956048
Amy C et al (2019) Advances in respiratory virus therapeutics - A meeting report from the 6th isirv Antiviral Group conference. Antiviral Res 167 45-67 PMID: 30974127
Martin et al (2014) mTORC1 and JNK coordinate phosphorylation of the p70S6K1 autoinhibitory domain in skeletal muscle following functional overloading. Am J Physiol Endocrinol Metab 306 E1397 PMID: 24801387
Varda et al (2022) Visual barcodes for clonal-multiplexing of live microscopy-based assays. Nat Commun 13 2725 PMID: 35585055
Steven A et al (2022) RNF43 G659fs is an oncogenic colorectal cancer mutation and sensitizes tumor cells to PI3K/mTOR inhibition. Nat Commun 13 3181 PMID: 35676246
Fuqin et al (2022) HCN1 channels mediate mu opioid receptor long-term depression at insular cortex inputs to the dorsal striatum. J Physiol 600 4917-4938 PMID: 36181477
Rinat R et al (2022) mTORC1 and mTORC2 Complexes Regulate the Untargeted Metabolomics and Amino Acid Metabolites Profile through Mitochondrial Bioenergetic Functions in Pancreatic Beta Cells. Nutrients 14 PMID: 35893876
Harari et al (2018) Direct Targeting of the mTOR (Mammalian Target of Rapamycin) Kinase Improves Endothelial Permeability in Drug-Eluting Stents-Brief Report. Arterioscler Thromb Vasc Biol 38 2217 PMID: 30026269
Feehan et al (2018) Inhibition of mTORC2 enhances UVB-induced apoptosis in keratinocytes through a mechanism dependent on the FOXO3a transcriptional target NOXA but independent of TRAIL. Cell Signal 52 35 PMID: 30172026
Zullo et al (2014) Mammalian target of Rapamycin inhibition and mycobacterial survival are uncoupled in murine macrophages. Cell 15 4 PMID: 24528777
Brown et al (2014) Mitogen-activated protein kinase-interacting kinase regulates mTOR/AKT signaling and controls the serine/arginine-rich protein kinase-responsive type 1 internal ribosome entry site-mediated translation and viral oncolysis. Mol Biol Cell 88 13149 PMID: 25187540
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*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
This product guide reviews some of the main areas in cancer metabolism research and lists around 150 products that can be used to investigate metabolic pathways in cancer including:
This poster summarizes the main metabolic pathways in cancer cells and highlights potential targets for cancer therapeutics. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways providing potential cancer therapeutic targets.