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Merck

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

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About This Item

Empirical Formula (Hill Notation):
C24H15F3N4O
Molecular Weight:
432.40
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥99% (HPLC)
Form:
powder
Quality level:
100
Storage condition:
OK to freeze, protect from light

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assay

≥99% (HPLC)

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

Quality Level

100

Related Categories

Disclaimer

Toxicity: Standard Handling (A)

Biochem/physiol Actions

Reversible: yes
Cell permeable: yes
Primary Target
MTOR

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 (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.

Other Notes

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

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

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.

Legal Information

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

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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