Torin 1  1222998-36-8

 Torin1
分子式：C35H28F3N5O2  分子量：607.64
 
產品描述
Torin 1 是有效的mTORC1/2抑制劑，IC50為2 nM/10 nM;作用于mTOR比作用于PI3K選擇性高1000倍。
靶點
mTOR
         
IC50
2-10 nM
         
體外研究
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 compley 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.
體內研究
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.
溶解性
DMSO  1 mM
穩定性
2年 -20°C粉狀，6月-80°C溶于DMSO