中文名 | 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 | 1-[4-[4-(1-Oxopropyl)-1-piperazinyl]-3-(trifluoromethyl)phenyl]-9-(3-quinolinyl)benzo[h]-1,6-naphthyridin-2(1H)-one |
别名 | 化合物TORIN 1 MTORC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 1 TORIN-1 CS-1958 TORIN 1 mTOR Inhibitor XI,Torin1-Calbiochem mTOR Inhibitor XI, Torin1 - Calbiochem 1-[4-(4-PROPANOYLPIPERAZIN-1-YL)-3-(TRIFLUOROMETHYL)PHENYL]-9-QUINOLIN-3-YLBENZO[H][1,6]NAPHTHYRIDIN-2-ONE 1-[4-[4-(1-Oxopropyl)-1-piperazinyl]-3-(trifluoromethyl)phenyl]-9-(3-quinolinyl)benzo[h]-1,6-naphthyridin-2(1H)-one Benzo[h]-1,6-naphthyridin-2(1H)-one, 1-[4-[4-(1-oxopropyl)-1-piperazinyl]-3-(trifluoromethyl)phenyl]-9-(3-quinolinyl)- 1-[4-[4-(1-Oxopropyl)-1-piperazinyl]-3-(trifluoromethyl)phenyl]-9-(3-quinolinyl)benzo[h]-1,6-naphthyridin-2(1H)-one Torin 1 |
CAS | 1222998-36-8 |
化学式 | C35H28F3N5O2 |
分子量 | 607.62 |
密度 | 1.362 |
熔点 | >223°C (dec.) |
沸点 | 817.2±65.0 °C(Predicted) |
溶解度 | 溶于DMSO (高达8 mg/ml)。 |
酸度系数 | 4.19±0.20(Predicted) |
存储条件 | +2C to +8C |
稳定性 | 从提供的购买之日起稳定2年。DMSO中的溶液可以在-20 °C下储存长达2个月。 |
外观 | 黄白色粉末 |
颜色 | White or off-white |
物化性质 | 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。 |
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. 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 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. 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。 |
安全术语 | 24/25 - 避免与皮肤和眼睛接触。 |
海关编号 | 29334900 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.646 ml | 8.229 ml | 16.458 ml |
5 mM | 0.329 ml | 1.646 ml | 3.292 ml |
10 mM | 0.165 ml | 0.823 ml | 1.646 ml |
5 mM | 0.033 ml | 0.165 ml | 0.329 ml |
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