1222998-36-8
中文名称
1-[4-[4-(1-氧代丙基)-1-哌嗪基]-3-(三氟甲基)苯基]-9-(3-喹啉基)苯并[H]-1,6-萘啶-2(1H)-酮
英文名称
Torin 1
CAS
1222998-36-8
分子式
C35H28F3N5O2
分子量
608
MOL 文件
1222998-36-8.mol
更新日期
2024/04/22 14:02:28
1222998-36-8 结构式
基本信息
中文别名
化合物TORIN 1MTORC抑制剂(TORIN1)
1-[4-[4-(1-氧代丙基)-1-哌嗪基]-3-(三氟甲基)苯基]-9
1-[4-[4-(1-氧代丙基)-1-哌嗪基]-3-(三氟甲基)苯基]-9-(3-喹啉基)苯并[H]-1,6-萘啶-2(1H)-酮
英文别名
Torin 1CS-1958
Torin 1, >=98%
TORIN-1
TORIN 1
Torin 1 USP/EP/BP
mTOR Inhibitor XI, Torin1 - Calbiochem
Torin 1 - MTOR inhibitor,potent and selective
1-(4-(4-Propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naph
1-[4-(4-PROPANOYLPIPERAZIN-1-YL)-3-(TRIFLUOROMETHYL)PHENYL]-9-QUINOLIN-3-YLBENZO[H][1,6]NAPHTHYRIDIN-2-ONE
1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one
所属类别
生物化工：mTOR 抑制剂物理化学性质
熔点>223°C (dec.)
沸点817.2±65.0 °C(Predicted)
密度1.362
储存条件+2C to +8C
溶解度溶于DMSO（高达8mg/ml）。
酸度系数(pKa)4.19±0.20(Predicted)
形态黄白色粉末
颜色白色或灰白色
稳定性Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
常见问题列表
生物活性
Torin 1是一种有效的mTORC1/2抑制剂，IC50为2 nM/10 nM；作用于mTOR比作用于PI3K选择性高1000倍。体外研究
Torin1 inhibits phosphorylation of mTORC1 and mTORC2 substrates in cells at concentrations of 2 and 10 nM, respectively. Moreover, Torin1 exhibits 1000-fold selectivity for mTOR over PI3K (EC50 = 1800 nM) and exhibits 100-fold binding selectivity relative to 450 other protein kinases. Torin1 causes cell cycle arrest through a rapamycin-resistant mechanism that is also independent of mTORC2. Torin1 disrupts mTORC1-dependent phenotypes more completely than rapamycin. Rapamycin-resistant functions of mTORC1 are required for cap-dependent translation. In a recent study, it is reported Torin1 increases neurotensin secretion and gene expression through activation of the MEK/ERK/c-Jun pathway in the human endocrine cell line BON.体内研究
Torin1 is efficacious at a dose of 20 mg/kg in a U87MG xenograft model and demonstrates good pharmacodynamic inhibition of downstream effectors of mTOR in tumor and peripheral tissues.生物活性
Torin 1是一种有效的mTORC1/2抑制剂，在无细胞试验中IC50为2 nM/10 nM；作用于mTOR比作用于PI3K选择性高1000倍。靶点
| Target | Value |
|
mTORC1
(Cell-free assay) | 2 nM |
|
mTOR
(Cell-free assay) | 4.32 nM |
|
DNA-PK
(Cell-free assay) | 6.34 nM |
|
mTORC2
(Cell-free assay) | 10 nM |
|
p110γ
(Cell-free assay) | 171 nM |
体外研究
Torin1在2和10 nM浓度下分别抑制mTORC1 和mTORC2底物的磷酸化。此外，Torin1对mTOR比对PI3K (EC50 = 1800 nM)的选择性高1000倍，比对450种其它蛋白激酶的结合选择性高100倍。 Torin1通过耐rapamycin机制引起细胞周期阻滞，并且其不依赖于mTORC2。Torin1比rapamycin更完全地干扰mTORC1依赖表现型。Cap依赖性翻译需要mTORC1耐Rapamycin的功能。在近期的一项研究中，据报道Torin1通过活化人内分泌细胞系BON 中MEK/ERK/c-Jun通路，能够增加神经降压素分泌和基因表达。
体内研究
Torin1在20 mg/kg剂量下，在U87MG异种移植模型中是有效的，并且在肿瘤和外周组织中对mTOR下游效应蛋白表现出良好的药效学抑制作用。1-[4-[4-(1-氧代丙基)-1-哌嗪基]-3-(三氟甲基)苯基]-9-(3-喹啉基)苯并[H]-1,6-萘啶-2(1H)-酮价格(试剂级)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2024/01/25 | HY-13003 | 1-[4-[4-(1-氧代丙基)-1-哌嗪基]-3-(三氟甲基)苯基]-9-(3-喹啉基)苯并[H]-1,6-萘啶-2(1H)-酮 Torin 1 | 1222998-36-8 | 5mg | 770元 |
| 2024/01/25 | HY-13003 | 1-[4-[4-(1-氧代丙基)-1-哌嗪基]-3-(三氟甲基)苯基]-9-(3-喹啉基)苯并[H]-1,6-萘啶-2(1H)-酮 Torin 1 | 1222998-36-8 | 10mg | 1252元 |
| 2024/01/25 | HY-13003 | 1-[4-[4-(1-氧代丙基)-1-哌嗪基]-3-(三氟甲基)苯基]-9-(3-喹啉基)苯并[H]-1,6-萘啶-2(1H)-酮 Torin 1 | 1222998-36-8 | 50mg | 4000元 |