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Torin 1

Torin 1

产品编号 T6045   CAS 1222998-36-8

Torin 1 是一种有效的 mTOR 抑制剂,IC50为 3 nM。它抑制 mTORC1/2复合物的 IC50值在 2 和 10 nM 之间,还诱导自噬

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Torin 1, CAS 1222998-36-8
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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 effective inhibitor of mTORC1/2 with (IC50: 2 nM/10 nM); has 1000-fold selectivity for mTOR than PI3K.
靶点活性 mTORC1:2 nM, mTORC2:10 nM
体外活性 Torin1(20 mg/kg)对U87 mg异种移植模型有效的,且可有效抑制肿瘤和外周组织中的mTOR下游效应蛋白.
体内活性 Torin1通过耐雷帕霉素机制引起细胞周期阻滞,并且其不依赖于mTORC2。Torin1比雷帕霉素对mTORC1依赖的表现型干扰更完全。在近期的一项研究中表明,Torin1通过活化人内分泌细胞系BON 中MEK/ERK/c-Jun通路,能够增加神经降压素分泌和基因表达。Torin1(2、10 nM)可分别抑制mTORC1 和mTORC2底物的磷酸化。
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 2 years

溶解度

DMSO: 2.5 mM

( < 1 mg/mL refers to the product slightly soluble or insoluble )

参考文献

1. Thoreen CC, et al, J Biol Chem, 2009, 284(12), 8023-8032. 2. Liu Q, et al, J Med Chem, 2010, 53(19), 7146-7155. 3. Li J, et al, Am J Physiol Cell Physiol, 2011, 301(1), C213-C226. 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.

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.
Duvelisib (R enantiomer) hydrochloride PI3K/Akt/mTOR-IN-2 TGX-115 PI3Kα/mTOR-IN-1 Urea, N-[4-[4-(8-oxa-3-azabicyclo[3.2.1]oct-3-yl)thieno[3,2-d]pyrimidin-2-yl]phenyl]-N'-3-pyridinyl- Torbafylline PI5P4Ks-IN-2 GSK2292767 FA

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 DNA 损伤和修复分子库 神经元分化化合物库 抗胰腺癌化合物库 激酶抑制剂库 糖代谢化合物库 已知活性化合物库 细胞焦亡化合物库 癌细胞分化化合物库 抗结直肠癌化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
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计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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技术支持

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 PI3K DNA-PK mTOR Mammalian target of Rapamycin Torin1 Inhibitor Torin-1 inhibit inhibitor

 

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