85-2074-69　［取扱停止］mTOR Inhibitor XI, Torin1 (1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one, DNA-PK Inhibitor VI, PI 3-K Inhibitor XVIII) 10mg　217571

特徴

• A cell-permeable pyridinonequinoline derivative that acts as a highly potent, ATP-competitive inhibibitor against mTOR and DNA-PK (IC50 = 4.32 and 6.34nM, respectively), while inhibiting PI 3-K only at much higher concentrations (IC50 =171 to 533nM). Effectively inhibits mTORC1-mediated S6K1 phosphorylation in MEF (IC50 = 2nM) in vitro, as well as mTORC2-mediated Akt and mTORC1-dependent S6 phosphorylations in murine lung and liver in vivo (up to 6h post single 20mg/kg i.p. dose). Despite its poor in vivo stability (T1/2 = 4.52h in mice; 10mg/kg i.p.), Torin1 is reported to completely suppress U87MG-derived tumor expansion in mice when administered via daily i.p. at a high dosage of 200mg/kg. Also reported to effectively inhibit cellular mTORC1 functionalities known to be rapamycin-resistant.
• Primary Target:MTOR
• Primary Target IC50:2nM
• Molar Mass:607.62
• Solubility:DMSO
• Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.