A Torin1 structural analog that acts as a cell-permeable, potent, ATP-competitive inhibitor against DNA-PK and mTOR (IC50 = 0.5 and 2.81nM, respectively). Comparing to Torin1, Torin2 displays enhanced inhibitory potency against PI 4-Kbeta (IC50 = 18.3nM) and PI 3-K (IC50 =4.68, 5.67, 8.58, 17.5, 24.5, and 28.1nM, respectively, against P110alpha/P85alpha, P110-gamma, hVPS34, P110delta/P85alpha, C2beta, C2alpha, respectively), while being more effective in inhibiting S6K1 Thr389 phosphorylation in MEF cultures (IC50 = 0.25nM vs 2nM, respectively, for Torin2 and Torin1) in vitro and displaying much improved oral bioavailability in mice (Cmax (ng/mL) /T1/2 (h) = 3968/0.72 and 223/0.79, respectively, for Torin2 and Torin1; 10/mg/kg p.o.) in vivo.
Molecular Formula:C₂₄H₁₅F₃N₄O
Primary Target:MTOR
Primary Target IC50:2nM
Molecular Weight:432.4
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.