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Torin 1

Torin 1

产品编号 T6045   CAS 1222998-36-8

Torin 1 是一种 mTOR 抑制剂,可以抑制 mTORC1 和 mTORC2 (IC50=2/10 nM),具有选择性和 ATP 竞争性。Torin 1 可以诱导细胞自噬,具有抗肿瘤、抗炎、抗衰老活性。

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Torin 1 Chemical Structure
Torin 1, CAS 1222998-36-8
规格 价格/CNY 货期 数量
1 mg ¥ 273 现货
2 mg ¥ 389 现货
5 mg ¥ 637 现货
10 mg ¥ 987 现货
25 mg ¥ 1,930 现货
50 mg ¥ 3,290 现货
100 mg ¥ 3,990 现货
500 mg ¥ 8,880 现货
618惊喜特惠 4重福利大放送
药物设计专题培训
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
产品目录号及名称: Torin 1 (T6045)
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纯度: 99.38%
纯度: 99%
纯度: 98.3%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Torin 1 is an mTOR inhibitor that inhibits mTORC1 and mTORC2 (IC50=2/10 nM) selectively and ATP-competitively. Torin 1 induces cellular autophagy and possesses anti-tumor, anti-inflammatory, and anti-aging activities.
靶点活性 mTORC2:10 nM, mTORC1:2 nM
体外活性 方法:野生型 MEFs 细胞用 Torin 1 (250 nm) 处理 4 天,使用 CellTiterGlo viability assay 检测细胞增殖。
结果:250 nm Torin1 完全抑制细胞增殖。[1]
方法:人类内分泌细胞系 BON 用 Torin 1 (62.5-150 µM) 处理 3-24 h,使用 Western Blot 检测靶点蛋白表达水平。
结果:Torin1 以剂量依赖的方式增加 NT 分泌;在 Torin1 处理后 3-24 h,NT 分泌增加。Torin1 处理降低了 Akt (S473) 磷酸化,p70S6K (T389) 以及 4E-BP1 (T37/46) 的磷酸化也受到抑制。[2]
体内活性 方法:为检测体内抗肿瘤活性,将 Torin 1 (20 mg/kg,20% N-mentyl-2-pyrrolidone, 40% PEG400 and 40% water) 腹腔注射给携带人胶质母细胞瘤 U87MG 的 NCR nude 小鼠,每天一次,持续十天。
结果:连续给药十天导致大于 99% 的肿瘤生长抑制。停止药物治疗后,肿瘤继续生长,这表明 Torin 1 治疗主要是细胞抑制性的,并且大量肿瘤细胞在治疗过程中仍然存活。[3]
激酶实验 mTORC1 and mTORC2 in Vitro Kinase Assays: To produce soluble mTORC1, HEK-293T cell lines that stably express N-terminally FLAG-tagged Raptor are generated using vesicular stomatitis virus G-pseudotyped MSCV retrovirus. For mTORC2, similar HeLa cells that stably express N-terminally FLAG-tagged Protor-1 are generated. Both complexes are purified by lysing cells in 50 mm HEPES, pH 7.4, 10 mm sodium pyrophosphate, 10 mm sodium β-glycerophosphate, 100 mm NaCl, 2 mm EDTA, 0.3% CHAPS. Cells are lysed at 4 °C for 30 min, and the insoluble fraction is removed by microcentrifugation at 13,000 rpm for 10 min. Supernatants are incubated with FLAG-M2 monoclonal antibody-agarose for 1 h and then washed three times with lysis buffer and once with lysis buffer containing a final concentration of 0.5 M NaCl. Purified mTORC1 is eluted with 100 μg/mL 3×FLAG peptide in 50 mm HEPES, pH 7.4, 100 mm NaCl. Eluate can be aliquoted and stored at -80 °C. Substrates S6K1 and Akt1 are purified. Kinase assays are performed for 20 min at 30 °C in a final volume of 20 μL consisting of the kinase buffer (25 mm HEPES, pH 7.4, 50 mm KCl, 10 mm MgCl2, 500 μm ATP) and 150 ng of inactive S6K1 or Akt1 as substrates. Reactions are stopped by the addition of 80 μL of sample buffer and boiled for 5 min. Samples are subsequently analyzed by SDS-PAGE and immunoblotting.
细胞实验 Cell viability is assessed with the CellTiter-Glo Luminescent Cell Viability Assay. On Day 0, 96-well plates are seeded with 500 cells per well and grown overnight. On Day 1, cells are treated with the appropriate compounds and subsequently analyzed on Days 3-5. For analysis, plates are incubated for 60 min at room temperature; 50 μL of CellTiter-Glo reagent is added to each well, and plates are mixed on an orbital shaker for 12 min. Luminescence is quantified on a standard plate luminometer. (Only for Reference)
分子量 607.62
分子式 C35H28F3N5O2
CAS No. 1222998-36-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 1mg/ml, Sonication is recommended.

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TargetMol Library Books参考文献

1. Thoreen CC, et al. An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORCJ Biol Chem. 2009 Mar 20;284(12):8023-32. 2. Li J, et al. mTORC1 inhibition increases neurotensin secretion and gene expression through activation of the MEK/ERK/c-Jun pathway in the human endocrine cell line BON. Am J Physiol Cell Physiol. 2011 Jul;301(1):C213-26. 3. Liu Q, et al. Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer. J Med Chem. 2010 Oct 14;53(19):7146-55. 4. Dowling RJ, et al, Science, 2010, 328(5982), 1172-1176. 5. Mitra D, Vega‐Rubin‐de‐Celis S, Royla N, et al. Abrogating GPT2 in triple negative breast cancer inhibits tumor growth and promotes autophagy[J]. International Journal of Cancer. 6. Mitra D, Vega‐Rubin‐de‐Celis S, Royla N, et al. Abrogating GPT2 in triple‐negative breast cancer inhibits tumor growth and promotes autophagy[J]. International Journal of Cancer. 2021, 148(8): 1993-2009. 7. Lu X Y, Shi X J, Hu A, et al. Feeding induces cholesterol biosynthesis via the mTORC1–USP20–HMGCR axis[J]. Nature. 2020, 588(7838): 479-484.

TargetMol Library Books文献引用

1. Lu X Y, Shi X J, Hu A, et al. Feeding induces cholesterol biosynthesis via the mTORC1–USP20–HMGCR axis. Nature. 2020, 588(7838): 479-484. 2. Sun C Y, Li Y Z, Cao D, et al. Rapamycin and trametinib: a rational combination for treatment of NSCLC. International Journal of Biological Sciences. 2021, 17(12): 3211-3223. 3. Mitra D, Vega‐Rubin‐de‐Celis S, Royla N, et al. Abrogating GPT2 in triple-negative breast cancer inhibits tumor growth and promotes autophagy. International Journal of Cancer. 2021 Apr 15;148(8):1993-2009. 4. Zheng J, Deng Y, Wei Z, et al.Lipid phosphatase SAC1 suppresses hepatitis B virus replication through promoting autophagic degradation of virions.Antiviral Research.2023: 105601. 5. Huang Z, Zhu S, Han Z, et al.Proteome-Wide Analysis Reveals TFEB Targets for Establishment of a Prognostic Signature to Predict Clinical Outcomes of Colorectal Cancer.Cancers.2023, 15(3): 744. 6. Li L, Fu S, Wang J, et al.SRT1720 inhibits bladder cancer cell progression by impairing autophagic flux.Biochemical Pharmacology.2024: 116111. 7. Ying R, Li C, Li H, et al.RPGR is a guanine nucleotide exchange factor for the small GTPase RAB37 required for retinal function via autophagy regulation.Cell Reports.2024, 43(4): 114010.
KU-55933 LY294002 Wortmannin PIK-90 ETP-45658 PI3K-IN-1 PI-103 (Rac)-Nedisertib

相关化合物库

该产品包含在如下化合物库中:
高选择性抑制剂库 抑制剂库 激酶抑制剂库 抗乳腺癌化合物库 DNA 损伤和修复分子库 糖酵解化合物库 神经元分化化合物库 PI3K/Akt/mTOR 化合物库 氧化还原化合物库 细胞重编程化合物库

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Torin 1 1222998-36-8 Autophagy DNA Damage/DNA Repair PI3K/Akt/mTOR signaling mTOR PI3K DNA-PK Mammalian target of Rapamycin Torin1 Inhibitor Torin-1 inhibit inhibitor

 

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