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Torin 1 {[allProObj[0].p_purity_real_show]}

货号：A113194

Torin 1是一种高效的 mTOR 抑制剂，其 IC50 为 3 nM，抑制 mTORC1 和 mTORC2 复合物的 IC50 值在 2 至 10 nM 之间，是一种有效的自噬诱导剂。

Torin 1 化学结构 CAS号：1222998-36-8
Torin 1 化学结构
CAS号：1222998-36-8
Torin 1 3D分子结构
CAS号：1222998-36-8
Torin 1 化学结构 CAS号：1222998-36-8
Torin 1 3D分子结构 CAS号：1222998-36-8
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Torin 1 纯度/质量文件 产品仅供科研

货号：A113194 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

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更多 >
产品名称 mTOR ↓ mTORC1 ↓ mTORC2 ↓ 其他靶点 纯度
AZD-8055 ++++

mTOR (full length), IC50: 0.8 nM

mTOR (truncated), IC50: 0.13 nM

 		99%+
Gedatolisib ++++

mTOR, IC50: 1.6 nM

 		99%
GSK1059615 ++

mTOR, IC50: 12 nM

 		98%
Vistusertib +++

mTOR, IC50: 2.8 nM

 		99%+
Torin 1 +++

mTOR, IC50: 4.32 nM

 		+++

mTORC1, IC50: 2 nM

 		++

mTORC2, IC50: 10 nM

 		DNA-PK 99%+
Dactolisib +++

mTOR (p70S6K), IC50: 6 nM

 		98+%
PI-103 +

mTOR, IC50: 30 nM

 		99%+
WAY-600 ++

mTOR, IC50: 9 nM

 		99%
Voxtalisib +

mTOR, IC50: 157 nM

 		99%+
PF-04691502 ++

mTOR, Ki: 16 nM

 		98+%
Onatasertib ++

mTOR, IC50: 16 nM

 		DNA-PK 99%+
Chrysophanol ✔ EGFR 98%
Samotolisib ✔ DNA-PK 99%+
Torkinib +++

mTOR, IC50: 8 nM

 		DNA-PK,PDGFR 99%+
Everolimus 99%+
WYE-354 +++

mTOR, IC50: 5 nM

 		98%
Tacrolimus ✔ 98%
PP121 ++

mTOR, IC50: 13 nM

 		VEGFR,PDGFR 99%+
Torin 2 ++++

mTOR, IC50: 0.25 nM

 		DNA-PK 99%+
Rapamycin ++++

mTOR, IC50: ~0.1 nM

 		98%
GDC-0349 +++

mTOR, Ki: 3.8 nM

 		98%
XL388 ++

mTOR, IC50: 9.9 nM

 		+++

mTORC1, IC50: 8 nM

 		+

mTORC2, IC50: 166 nM

 		99%+
WYE-687 +++

mTOR, IC50: 7 nM

 		98%
Apitolisib +

mTOR, Ki app: 17 nM

 		98%+
WYE-132 ++++

mTOR, IC50: 0.19 nM

 		99%+
Sapanisertib ++++

mTOR, Ki: 1.4 nM

 		99%+
BGT226 maleate ✔ 99%+
ETP-46464 ++++

mTOR, IC50: 0.6 nM

 		DNA-PK 98%
PI3K-IN-1 +

mTOR, IC50: 157 nM

 		98+%
Zotarolimus +++

FKBP-12, IC50: 2.8 nM

 		98%
OSI-027 +++

mTOR, IC50: 4 nM

 		+

mTORC1, IC50: 22 nM

 		+

mTORC2, IC50: 65 nM

 		99%+
Ridaforolimus ++++

mTOR, IC50: 0.2 nM

 		99%+
Temsirolimus +

mTOR, IC50: 1.76 μM

 		95%
CZ415 ++

mTOR, pIC50: 8.07

 		99%+
SF2523 +

mTOR, IC50: 280 nM

 		DNA-PK 99%+
KU-0063794 ++

mTORC1, IC50: ~10 nM

 		++

mTORC2, IC50: ~10 nM

 		99%+
Omipalisib ++++

mTORC1, Ki: 0.18 nM

 		++++

mTORC2, Ki: 0.3 nM

 		99%+
Palomid 529 ✔ 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
产品名称 Autophagy ↓ 其他靶点 纯度
SBI-0206965 +++

ULK1, IC50: 108 nM

ULK2, IC50: 711 nM

 		95%
Hydroxychloroquine sulfate ✔ 99%
Valproic acid sodium ✔ HDAC 97%
PFK-015 ++

PFKFB3, IC50: 207 nM

 		99%+
MRT68921 HCl ++++

ULK1, IC50: 2.9 nM

ULK2, IC50: 1.1 nM

 		99%+
ROC-325 ✔ 99%+
Autophinib +++

Autophagy, IC50: 40 nM

 		99%
Lys05 ✔ 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Torin 1 生物活性

靶点

  • mTORC1

    mTORC1, IC50:2 nM

  • mTORC2

    mTORC2, IC50:10 nM

  • mTOR

    mTOR, IC50:4.32 nM
描述 In wild-type MEFs, Torin1 (250 nM) fully arrests proliferation, induces G1/S cell cycle arrest, and reduces cell size more significantly than 50 nM rapamycin[1]. Torin1 exhibits over 800-fold selectivity for mTOR over PI3Kis, demonstrating high specificity compared to other PIKK family kinases, except for DNA-PK[2].
体内研究

Torin1 (20 mg/kg, i.p.) shows efficacy in a U87MG xenograft model, displaying significant pharmacodynamic inhibition of downstream effectors of mTOR in both tumor and peripheral tissues[2].
体外研究

In wild-type MEFs, Torin1 (250 nM) fully arrests proliferation, induces G1/S cell cycle arrest, and reduces cell size more significantly than 50 nM rapamycin[1].

Torin1 exhibits over 800-fold selectivity for mTOR over PI3Kis, demonstrating high specificity compared to other PIKK family kinases, except for DNA-PK[2].
作用机制 Torin 1 is an ATP-competitive inhibitor.

Torin 1 细胞实验

Cell Line
Concentration Treated Time Description References
HEK293T cells 1 µM 4 hours To study the effect of mTOR inhibitors on BRAF T401 phosphorylation, results showed torin1 significantly suppressed pT401 levels. Cell Commun Signal. 2024 Sep 2;22(1):428.
HepG2 cells 5 µM 1 h Torin 1 significantly increased rAAV-mediated transgene expression, indicating that induction of autophagy enhances rAAV transduction efficiency. Hepatology. 2017 Jul;66(1):252-265.
PHHs (primary human hepatocytes) 10 µM 1 h Torin 1 significantly increased rAAV-mediated transgene expression, indicating that induction of autophagy enhances rAAV transduction efficiency. Hepatology. 2017 Jul;66(1):252-265.
IMR90 cells 250 nM 24 h To investigate the effect of Torin 1 on SIRT1 expression under starvation and senescence conditions. Results showed that Torin 1 treatment suppressed the induction of LC3-II levels. Nat Cell Biol. 2020 Oct;22(10):1170-1179.
IMR90 cells 250 nM 24 h To investigate the effect of Torin 1 treatment on LC3 nuclear localization. Results showed that Torin 1 treatment increased LC3 localization in the cytoplasm. Nat Cell Biol. 2020 Oct;22(10):1170-1179.
Ba/F3-NRAS-G12D cells 300 nM 2 days Screen for compounds that potentiate the efficacy of Torin 1 against NRAS-driven cells Leukemia. 2015 Jan;29(1):27-37.
LHCN-M2 human skeletal muscle cells 250 nM 2 h Torin 1 completely prevented the reduction in PGC-1α expression caused by tunicamycin, suggesting the involvement of mTOR in the reduction of PGC-1α expression Cell Commun Signal. 2022 Apr 15;20(1):53.
LHCN-M2 human skeletal muscle cells 250 nM 16 h Torin 1 prevented the reduction in PGC-1α protein levels caused by tunicamycin Cell Commun Signal. 2022 Apr 15;20(1):53.
Ba/F3-NRAS-G12D cells 20 nM 2 days To identify compounds that synergize with Torin 1 and validate the synergy between MK-1775 and mTOR inhibitors Leukemia. 2015 Jan;29(1):27-37.

Torin 1 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Healthy mice Intraperitoneal injection 20 mg/kg Single dose, lasting 2 hours Torin 1 significantly increased rAAV8-TTR-Epo-mediated hepatic gene expression, indicating that induction of autophagy enhances rAAV transduction efficiency in vivo. Hepatology. 2017 Jul;66(1):252-265.
Mice C57BL/6 mice Intraperitoneal injection 5 mg/kg Single injection, sacrificed 24 hours later Torin 1 prevented the reduction in PGC-1α protein levels caused by tunicamycin Cell Commun Signal. 2022 Apr 15;20(1):53.

Torin 1 动物研究

Dose Mice: 1 mg/kg[3] (i.v.), 10 mg/kg[3] (i.p./p.o.), 20 mg/kg[3] (i.p.)
Administration i.v., i.p., p.o.
Pharmacokinetics
Animal Nude mice[3]
Dose 1 mg/kg (i.v.)
10 mg/kg (p.o. or i.p.)
MRT 0.43 h (i.v.)
1.51 h (p.o.)
F 5.49% (p.o.)
T1/2 0.5 h (i.v.)
0.79 h (p.o.)
4.52 h (i.p.)
Tmax 0.25 h (p.o.)
0.08 h (i.p.)
Vss 0.59 L/kg (i.v.)
Cmax 2757 ng/ml (i.v.)
223 ng/ml (p.o.)
5121 ng/ml (i.p.)
CL 23.0 ml/min/kg (i.v.)
AUC 720 h·ng/ml (i.v.)
396 h·ng/ml (p.o.)
5718 h·ng/ml (i.p.)

Torin 1 参考文献

[1]Thoreen CC, et al, An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1. J Biol Chem, 2009, 284(12), 8023-8032.

[2]Liu Q, et al. 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 Che

Torin 1 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.65mL

0.33mL

0.16mL

8.23mL

1.65mL

0.82mL

16.46mL

3.29mL

1.65mL

Torin 1 技术信息

CAS号1222998-36-8
分子式C35H28F3N5O2
分子量 607.62
SMILES Code O=C1N(C2=CC=C(N3CCN(C(CC)=O)CC3)C(C(F)(F)F)=C2)C4=C(C=NC5=CC=C(C6=CC7=CC=CC=C7N=C6)C=C54)C=C1
MDL No. MFCD18782653
别名
运输蓝冰
InChI Key AKCRNFFTGXBONI-UHFFFAOYSA-N
Pubchem ID 49836027
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C
溶解方案

DMSO: 2 mg/mL(3.29 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Torin 1 | 1222998-36-8 | Torin1 | Torin-1 | mTOR Inhibitor | PI3K/Akt/mTOR | Autophagy | mTOR | Autophagy | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Torin 1 纯度/质量文件 | Torin 1 亚型比较 | Torin 1 生物活性 | Torin 1 动物研究 | Torin 1 参考文献 | Torin 1 实验方案 | Torin 1 技术信息

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