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Merck
CN

475991

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
化学文摘社编号:
1222998-36-8
分子量:
607.62
MDL number:
MFCD18782653
UNSPSC Code:
12352200
NACRES:
NA.77

主要文件

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产品名称

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).

SMILES string

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

assay

≥99% (HPLC)

form

powder

potency

2 nM IC50

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

yellow-white

solubility

DMSO: 2 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

100

相关类别

Biochem/physiol Actions

主要靶标
MTOR
可逆性：是
细胞可渗透性：具有

Disclaimer

毒性：标准处理（A）

General description

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）。

Other Notes

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

Packaging

用惰性气体包装

Preparation Note

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。

Legal Information

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

存储类别

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

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