MilliporeSigma™ Calbiochem™ mTOR Inhibitor XII, Torin2

Description

• A Torin1 (Cat
• No
• 475991) structural analog that acts as a cell-permeable, potent, ATP-competitive inhibitor against DNA-PK and mTOR (IC 50 = 0.5 and 2.81 nM, respectively)
• Comparing to Torin1, Torin2 displays enhanced inhibitory potency against PI 4-Kβ (IC 50 = 18.3nM) and PI 3-K (IC 50 =4.68, 5.67, 8.58, 17.5, 24.5, and 28.1 nM, respectively, against P110α/P85α, P110γ, hVPS34, P110δ/P85α, C2β, C2α, respectively), while being more effective in inhibiting S6K1 Thr389 phosphorylation in MEF cultures (IC 50 = 0.25nM vs 2 nM, respectively, for Torin2 and Torin1) in vitro and displaying much improved oral bioavailability in mice ( C max (ng/mL) / T 1/2 (h) = 3968/0.72 and 223/0.79, respectively, for Torin2 and Torin1; 10 /mg/kg p.o.) in vivo .