Torin 1
(Synonyms: 1-[4-[4-(1-氧代丙基)-1-哌嗪基]-3-(三氟甲基)苯基]-9-(3-喹啉基)苯并[H]-1,6-萘啶-2(1H)-酮,Torin1;Torin-1) 目录号 : GC10131
Torin 1是一种有效的ATP竞争性哺乳动物雷帕霉素靶蛋白（mTOR）抑制剂，IC50值为3nM。
Cas No.:1222998-36-8
Sample solution is provided at 25 µL, 10mM.
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Torin 1 is a potent ATP-competitive mammalian target of rapamycin (mTOR) inhibitor with an IC50 value of 3nM[1]. Torin 1 inhibits both mTORC1/2 complexes with IC50 values between 2 and 10nM[2]. Torin 1 is a potent autophagy inducer[3].
In vitro, treatment of glioblastoma (GB) LN-18 cells with Torin 1 (300, 1000nM) for 24h dose-dependently inhibited cell proliferation and migration and significantly inhibited cell entry into the S phase[4]. Treatment of S. pombe cells with Torin 1 (25μM) for 24h inhibited cell growth but did not cause cell death or G1 phase arrest[5].
In vivo, oral treatment of mice with dextran sulfate sodium (DSS)-induced colitis with Torin 1 (10, 20mg/kg) for 6 days significantly reduced pathological damage in the colon tissue and inhibited the production of proinflammatory cytokines in mice[6]. Torin 1 (400nM, 0.5μL) injected bilaterally into the insular cortex (IC) of nerve-injured rats significantly alleviated neuropathic pain and inhibited the increase in phosphorylated p70S6K (p-p70S6K) levels[7].
References:
[1] Thoreen C C, Kang S A, Chang J W, et al. An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1[J]. Journal of Biological Chemistry, 2009, 284(12): 8023-8032.
[2] Sun S Y. mTOR kinase inhibitors as potential cancer therapeutic drugs[J]. Cancer letters, 2013, 340(1): 1-8.
[3] Xu S, Li L, Li M, et al. Impact on autophagy and ultraviolet B induced responses of treatment with the MTOR inhibitors rapamycin, everolimus, torin 1, and pp242 in human keratinocytes[J]. Oxidative medicine and cellular longevity, 2017, 2017(1): 5930639.
[4] Amin A G, Jeong S W, Gillick J L, et al. Targeting the mTOR pathway using novel ATP-competitive inhibitors, Torin1, Torin2 and XL388, in the treatment of glioblastoma[J]. International journal of oncology, 2021, 59(4): 83.
[5] Atkin J, Halova L, Ferguson J, et al. Torin1-mediated TOR kinase inhibition reduces Wee1 levels and advances mitotic commitment in fission yeast and HeLa cells[J]. Journal of cell science, 2014, 127(6): 1346-1356.
[6] Liu T, Zheng S, Guo P. Effect of Torin 1 on suppressing inflammation in mice with dextran sodium sulfate-induced colitis[J]. Int J Clin Exp Med, 2017, 10(3): 4723-4731.
[7] Choi S, Kim K, Cha M, et al. mTOR signaling intervention by Torin1 and XL388 in the insular cortex alleviates neuropathic pain[J]. Neuroscience Letters, 2020, 718: 134742.
Torin 1是一种有效的ATP竞争性哺乳动物雷帕霉素靶蛋白（mTOR）抑制剂，IC50值为3nM[1]。Torin 1抑制两种mTORC1/2复合物，IC50值在2和10nM之间[2]。Torin 1是一种有效的自噬诱导剂[3]。
在体外，Torin 1（300, 1000nM）处理胶质母细胞瘤（GB） LN-18细胞24h，剂量依赖性地抑制了细胞增殖和迁移，并显著抑制了细胞进入S期[4]。Torin 1（25μM）处理S. pombe细胞24h，抑制了细胞的生长，但不会造成细胞死亡或G1期阻滞[5]。
在体内，Torin 1（10, 20mg/kg）通过口服治疗葡聚糖硫酸钠（DSS）诱导的结肠炎小鼠6天，显著减轻了小鼠结肠组织的病理损伤，抑制了促炎细胞因子的产生[6]。Torin 1（400nM, 0.5μL）通过双侧注射到神经损伤大鼠的岛叶皮层（IC），显著减轻了神经性疼痛，抑制了磷酸化p70S6K（p-p70S6K）水平的升高[7]。
| Cell experiment [1]: | |
Cell lines | LN-18 cells |
Preparation Method | Cells were treated with two doses (300 and 1000nM) of Torin 1, Torin 2, or XL388 for 24h, and then MTT assay was performed to measure cell proliferation. |
Reaction Conditions | 300, 1000nM; 24h |
Applications | Cell proliferation was significantly inhibited by Torin 1 in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | Mice were given free access to water containing Dextran sulfate sodium (DSS) for 6 days. The mice were randomly assigned to control, Torin 1 (20mg/kg)-treated, DSS-treated, Torin 1 (10mg/kg) +DSS-treated and Torin 1 (20mg/kg)+DSS-treated groups. Torin-1 as a suspension in 20% N-methyl-2-pyrrolidone/40% PEG400/40% water, orvehicle was delivered intragastrically once per day for 6 days from the first day, respectively. |
Dosage form | 10, 20mg/kg for 6 days; p.o. |
Applications | Torin 1 treatment significantly attenuated body weight loss and reduced the mortality induced by DSS. Torin 1 prevented DSS-induced colonic pathological damage, inhibited the production of pro-inflammatory cytokines in colon tissues. |
References: | |
| Cas No. | 1222998-36-8 | SDF | |
| 别名 | 1-[4-[4-(1-氧代丙基)-1-哌嗪基]-3-(三氟甲基)苯基]-9-(3-喹啉基)苯并[H]-1,6-萘啶-2(1H)-酮,Torin1;Torin-1 | ||
| 化学名 | 1-[4-(4-propanoylpiperazin-1-yl)-3-(trifluoromethyl)phenyl]-9-quinolin-3-ylbenzo[h][1,6]naphthyridin-2-one | ||
| Canonical SMILES | CCC(=O)N1CCN(CC1)C2=C(C=C(C=C2)N3C(=O)C=CC4=CN=C5C=CC(=CC5=C43)C6=CC7=CC=CC=C7N=C6)C(F)(F)F | ||
| 分子式 | C35H28F3N5O2 | 分子量 | 607.64 |
| 溶解度 | <1.22mg/mL in DMSO, ≥ 2.42 mg/mL in EtOH with ultrasonic and warming | 储存条件 | Desiccate at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6457 mL | 8.2286 mL | 16.4571 mL |
| 5 mM | 0.3291 mL | 1.6457 mL | 3.2914 mL |
| 10 mM | 0.1646 mL | 0.8229 mL | 1.6457 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
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- SDS (Safety Data Sheet)
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