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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 mTORC1mTORC2 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]}
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产品名称 mTOR mTORC1 mTORC2 其他靶点 纯度
AZD-8055 ++++

mTOR (truncated), IC50: 0.13 nM

mTOR (full length), IC50: 0.8 nM

99%+
Gedatolisib ++++

mTOR, IC50: 1.6 nM

98%
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

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

mTOR, IC50: 5 nM

98%
Tacrolimus 98%
PP121 ++

mTOR, IC50: 13 nM

PDGFR,VEGFR 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

99+%
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

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

PFKFB3, IC50: 207 nM

99%+
MRT68921 hydrochloride ++++

ULK1, IC50: 2.9 nM

ULK2, IC50: 1.1 nM

99%+
ROC-325 99%+
Autophinib +++

Autophagy, IC50: 40 nM

97%
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 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
697 Growth Inhibition Assay IC50=0.00634 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=0.04629 μM SANGER
A101D Growth Inhibition Assay IC50=0.0265 μM SANGER
A253 Growth Inhibition Assay IC50=0.98885 μM SANGER

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 607.624
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C

溶解度

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

动物实验配方
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