475992

mTOR Inhibitor XII, Torin2

• Synonym(s): mTOR Inhibitor XII, Torin2, 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one, DNA-PK Inhibitor VII, PI 3-K Inhibitor XIX, PI 4-K Inhibitor
• Empirical Formula (Hill Notation): C₂₄H₁₅F₃N₄O
• Molecular Weight: 432.40
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• assay: ≥99% (HPLC)
• Quality Level: 100
• form: powder
• potency: 2 nM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: yellow
• solubility: DMSO: 10 mg/mL
• shipped in: wet ice
• storage temp.: 2-8°C

Description

General description

A Torin1 (Cat. No. 475991) structural analog that acts as a cell-permeable, potent, ATP-competitive inhibitor against DNA-PK and mTOR (IC₅₀ = 0.5 and 2.81 nM, respectively). Comparing to Torin1, Torin2 displays enhanced inhibitory potency against PI 4-Kβ (IC₅₀ = 18.3 nM) and PI 3-K (IC₅₀ =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 (IC₅₀ = 0.25 nM 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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
MTOR

Reversible: yes

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Liu, Q., et al. 2011. J Med Chem.54, 1473.

Liu, Q., et al. 2010, J Biol Chem.284, 8023.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable