MilliporeSigma™ Calbiochem™ mTOR Inhibitor XI, Torin1

Description

A cell-permeable pyridinonequinoline derivative that acts as a highly potent, ATP-competitive inhibibitor against mTOR and DNA-PK (IC₅₀ = 4.32 and 6.34 nM, 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 6 h post single 20mg/kg i.p. dose). Despite its poor in vivo stability (T_1/2 = 4.52 h 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 (Cat. Nos. 553210, 553211, and 553212).