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Merck
CN

475991

Sigma-Aldrich

Torin1

≥99% (HPLC), powder, mTOR inhibitor, Calbiochem®

别名:

mTOR抑制剂XI，Torin1, 1-（4-（4-丙酰基哌嗪-1-基）-3-（三氟甲基）苯基）-9-（喹啉-3-基）苯并[h][1，6]萘啶-2（1h）-酮，DNA-PK抑制剂VI，PI 3-K抑制剂XVIII

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关于此项目

经验公式（希尔记法）:
C35H28F3N5O2
CAS Number:
1222998-36-8
分子量:
607.62
MDL编号:
MFCD18782653
UNSPSC代码:
12352200
NACRES:
NA.77

主要文件

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Product Name

mTOR抑制剂XI，Torin1, mTOR Inhibitor XI, Torin1, CAS 1222998-36-8, is a cell-permeable, highly potent, ATP-competitive inhibitor of mTOR and DNA-PK (IC50 = 4.32 and 6.34 nM, respectively).

质量水平

100

方案

≥99% (HPLC)

表单

powder

效能

2 nM IC50

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
protect from light

颜色

yellow-white

溶解性

DMSO: 2 mg/mL

运输

ambient

储存温度

2-8°C

SMILES字符串

FC(F)(F)c1c(ccc(c1)[n]3c4c5c(ncc4cc[c]3=O)ccc(c5)c6cnc7c(c6)cccc7)N2CCN(CC2)C(=O)CC

InChI

1S/C35H28F3N5O2/c1-2-32(44)42-15-13-41(14-16-42)31-11-9-26(19-28(31)35(36,37)38)43-33(45)12-8-24-20-40-30-10-7-22(18-27(30)34(24)43)25-17-23-5-3-4-6-29(23)39-21-25/h3-12,17-21H,2,13-16H2,1H3

InChI key

AKCRNFFTGXBONI-UHFFFAOYSA-N

相关类别

一般描述

一种可渗透细胞的吡啶酮喹啉衍生物，可作为针对mTOR和DNA-PK的高效，ATP竞争性抑制剂（在无细胞激酶测定中，IC50分别为4.32和6.34 nM），仅在更高的浓度下抑制I类（P110γ，P110α/P85α，和P110δ/P85α的IC50分别为171，250和564 nM），II类（C2α和C2β的IC50分别为176和564 nM）和III类（hVPS34的IC50=533 nM）PI 3-K。有效抑制体外MEF培养物中mTORC1介导的S6K1 Thr389磷酸化（IC50=2 nM），以及体内鼠肺和肝中mTORC2介导的Akt Ser473和mTORC1依赖性S6 Ser235/236磷酸化（单次腹腔内注射剂量为20 mg/kg后长达6小时）。尽管其体内稳定性差（小鼠中T1/2 =4.52 h；10 mg/kg i.p.），但据报告，Torin1通过每日200 mg/kg的高剂量i.p.给药可完全抑制U87MG衍生的小鼠肿瘤扩张。还报告了可有效抑制已知对雷帕霉素具有抗性的细胞mTORC1功能（目录号553210、553211和553212M）。

生化/生理作用

主要靶标
MTOR
可逆性：是
细胞可渗透性：具有

包装

用惰性气体包装

制备说明

复溶后，等分并冷冻保存（-20&C）。贮备液在-20°C下可稳定保存至多3个月。

其他说明

Liu, Q., et al. 2010.J Med Chem.53, 7146.
Thoreen, C., et al. 2009.J Biol Chem.284, 8023.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

免责声明

毒性：标准处理（A）

储存分类代码

11 - Combustible Solids

WGK

WGK 2

闪点(°F)

Not applicable

闪点(°C)

Not applicable

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Cell reports methods, 1(4), 100052-100052 (2022-04-28)
Engineered synthetic biomolecular devices that integrate elaborate information processing and precisely regulate living cell behavior have potential in various applications. Although devices that directly regulate key biomolecules constituting inherent biological systems exist, no devices have been developed to control intracellular
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PLoS pathogens, 19(1), e1011080-e1011080 (2023-01-13)
Kaposi's sarcoma-associated herpesvirus (KSHV) causes the inflammatory and angiogenic endothelial cell neoplasm, Kaposi's sarcoma (KS). We previously demonstrated that the KSHV Kaposin B (KapB) protein promotes inflammation via the disassembly of cytoplasmic ribonucleoprotein granules called processing bodies (PBs). PBs modify
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The Journal of infectious diseases, 224(7), 1160-1169 (2020-02-16)
Human polyomaviruses can reactivate in transplant patients, causing nephropathy, progressive multifocal leukoencephalopathy, Merkel cell carcinoma, pruritic, rash or trichodysplasia spinulosa. Sirolimus and related mechanistic target of rapamycin (mTOR) inhibitors are transplant immunosuppressants. It is unknown if they directly reactivate polyomavirus
Jee-Yun Park et al.
Scientific reports, 11(1), 21119-21119 (2021-10-28)
Transcription factor EB (TFEB) is a master regulator of the autophagy-lysosomal pathway (ALP). Here, we cloned a novel splicing variant of TFEB, comprising 281 amino acids (hereafter referred to as small TFEB), and lacking the helix-loop-helix (HLH) and leucine zipper
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