9-(6-Amino-3-pyridinyl)-1-[3-(trifluoromethyl)phenyl]benzo[h]-1,6-naphthyridin-2(1H)-one

Description

Torin 2 is a potent and selective inhibitor of cellular mTOR activity (EC₅₀ = 0.3 nM). It shows more than 800-fold selectivity for mTOR over PI3K (EC₅₀ = 200 nM) and greater than 100-fold binding selectivity relative to 440 other protein kinases. Torin 2 has significantly improved bioavailability (54%), metabolic stability, and plasma exposure compared to torin 1 .

The Uses of 9-(6-Amino-3-pyridinyl)-1-[3-(trifluoromethyl)phenyl]benzo[h]-1,6-naphthyridin-2(1H)-one

Torin 2 is a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer.

The Uses of 9-(6-Amino-3-pyridinyl)-1-[3-(trifluoromethyl)phenyl]benzo[h]-1,6-naphthyridin-2(1H)-one

Torin2 has been used:

• to examine its effect on LC3B-II levels in BORCS5- KO cells
• to determine its potent activity (IC₅₀?less than 1 μM) against A2780-cis ovarian cancer cells
• in western blot analysis

Definition

ChEBI: Torin 2 is a member of the class of pyridoquinolines that is benzo[h][1,6]naphthyridin-2-one carrying additional 3-(trifluoromethyl)phenyl and 6-aminopyridin-3-yl substituents at positions 1 and 9 respectively. It is a potent inhibitor of mTOR and exhibits anti-cancer properties. It has a role as a mTOR inhibitor and an antineoplastic agent. It is an organofluorine compound, a pyridoquinoline, an aminopyridine and a primary amino compound.

Biochem/physiol Actions

Torin2 is a highly potent and selective ATP-competitive mTOR inhibitor. Torin2 has an IC50 of 0.25 nM and 800-fold greater selectivity for mTOR than PI3K.

Storage

Store at +4°C

References

[1] liu q, wang j, kang s a, et al. discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl) phenyl) benzo [h][1, 6] naphthyridin-2 (1 h)-one (torin2) as a potent, selective, and orally available mammalian target of rapamycin (mtor) inhibitor for treatment of cancer. journal of medicinal chemistry, 2011, 54(5): 1473-1480.