ChemicalBook Produktkatalog Bio- und Chemieingenieurwesen Inhibitoren PI3K / Akt / mTOR mTOR-Inhibitoren 9-(6-Amino-3-pyridinyl)-1-[3-(trifluoromethyl)phenyl]benzo[h]-1,6-naphthyridin-2(1H)-one

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

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

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

CAS-Nr1223001-51-1

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

CBNumberCB52534663

SummenformelC24H15F3N4O

Molgewicht432.4

MOL-Datei1223001-51-1.mol

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

Schmelzpunkt	>275° C (dec.)
Siedepunkt	623.7±55.0 °C(Predicted)
Dichte	1.427
storage temp.	2-8°C
Löslichkeit	Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly, Heated)
Aggregatzustand	powder
pka	5.66±0.26(Predicted)
Farbe	white to beige

Gefahreninformationscode (GHS)

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

Beschreibung
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 .
Verwenden
Torin 2 is a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer.
Verwenden
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.
Lager
Store at +4°C
Einzelnachweise
[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.

9-(6-Amino-3-pyridinyl)-1-[3-(trifluoromethyl)phenyl]benzo[h]-1,6-naphthyridin-2(1H)-one Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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