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Torin 1

现货
Catalog No.
A8312
MTOR抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 700.00
现货
25mg
¥ 2,700.00
现货

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Background

Torin 1, a tricyclic benzonaphthyridinone, is a potent and selective inhibitor of the mammalian target of rapamycin (mTOR) kinase, which is the catalytic subunit of two functionally distinct complexes and plays a pivotal role in the regulation of cell growth, proliferation and survival. Torin 1 directly inhibits the two mTOR-containing complexes, mTORC1 and mTORC2, through an ATP-competitive mechanism with half maximal inhibitory concentration IC50 of 2 nM and 10 nM respectively. Torin 1 has been found to impair cell growth and proliferation through a mechanism involving mTORC1 inhibition other than mTORC2 inhibition, in which the rapamycin-resistant functions of mTORC1 is suppressed.

References:
[1]Thoreen CC1, Kang SA, Chang JW, Liu Q, Zhang J, Gao Y, Reichling LJ, Sim T, Sabatini DM, Gray NS. An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1. J Biol Chem. 2009 Mar 20;284(12):8023-32. doi: 10.1074/jbc.M900301200. Epub 2009 Jan 15.
[2]Liu Q1, Chang JW, Wang J, Kang SA, Thoreen CC, Markhard A, Hur W, Zhang J, Sim T, Sabatini DM, Gray NS. 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. doi: 10.1021/jm101144f.

文献引用

Chemical Properties

Physical AppearanceA solid
StorageDesiccate at -20°C
M.Wt607.64
Cas No.1222998-36-8
FormulaC35H28F3N5O2
SynonymsTorin1;Torin-1
Solubility<1.22mg/mL in DMSO, ≥2.42 mg/mL in EtOH with ultrasonic and warming, <2.39 mg/mL in H2O
Chemical Name1-[4-(4-propanoylpiperazin-1-yl)-3-(trifluoromethyl)phenyl]-9-quinolin-3-ylbenzo[h][1,6]naphthyridin-2-one
SDFDownload SDF
Canonical SMILESCCC(=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
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验: [1]

细胞系

MEFs

制备方法

溶解度有限,若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应条件

4 days,1-6 h

实验结果

250 nM Torin1完全抑制细胞增殖,并诱导G1/S细胞周期停滞。此外,与50 nM rapamycin相比,250 nM Torin1使细胞大小降低到更大的程度。此外,与rapamycin相比,Torin1将mTORC1依赖的表型破坏的更充分。

动物实验: [2]

动物模型

U87-MG胶质母细胞瘤异种移植小鼠

给药剂量

每日一次,IP给药,20 mg/kg

制备方法

以25 mg/mL溶于100%N-甲基-2-吡咯烷酮中

实验结果

Torin1连续治疗10天,抑制大于99%的肿瘤生长。治疗停止后肿瘤继续生长,表明Torin1主要是细胞抑制的,并且大量的肿瘤细胞在治疗期间仍然存活。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

1. Thoreen CC, Kang SA, Chang JW et al. An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1. J Biol Chem. 2009 Mar 20;284(12):8023-32.

2. Liu Q, Chang JW, Wang J et al. Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benz

o[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.

生物活性

描述 Torin 1是一种有效的mTORC1/2抑制剂,IC50值分别为2 nM/10 nM。
靶点 mTOR          
IC50 2-10 nM          

质量控制

化学结构

Torin 1

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