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475992

mTOR Inhibitor XII, Torin2

Name: mTOR Inhibitor XII, Torin2
Brand: MM

Sinónimos:

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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Fórmula empírica (notación de Hill):

C₂₄H₁₅F₃N₄O

Peso molecular:

432.40

NACRES:

NA.77

UNSPSC Code:

12352200

Assay:

≥99% (HPLC)

Form:

powder

Storage condition:

OK to freeze, protect from light

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Propiedades

assay

≥99% (HPLC)

Quality Segment

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

Descripción

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)

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Este artículo	475991	475988	528111
Sigma-Aldrich 475992 mTOR Inhibitor XII, Torin2	Sigma-Aldrich 475991 mTOR Inhibitor XI, Torin1	Sigma-Aldrich 475988 mTOR Inhibitor III, PP242	Sigma-Aldrich 528111 PI 3-Kα Inhibitor IV
description -	description mTOR Inhibitor XI, Torin1, CAS 1222998-36-8, is a cell-permeable, highly potent, ATP-competitive inhibitor of mTOR and DNA-PK (IC50 = 4.32 and 6.34 nM, respectively).	description The mTOR Inhibitor III, PP242 controls the biological activity of mTOR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.	description The PI 3-Kα Inhibitor IV, also referenced under CAS 1188890-32-5, controls the biological activity of PI 3-Kα. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
assay ≥99% (HPLC)	assay ≥99% (HPLC)	assay ≥97% (HPLC)	assay ≥95% (HPLC)
form powder	form powder	form solid	form solid
manufacturer/tradename Calbiochem^®	manufacturer/tradename Calbiochem^®	manufacturer/tradename Calbiochem^®	manufacturer/tradename Calbiochem^®
Quality Level 100	Quality Level 100	Quality Level 100	Quality Level 100
storage temp. 2-8°C	storage temp. 2-8°C	storage temp. −20°C	storage temp. 2-8°C
storage condition OK to freeze, protect from light	storage condition protect from light, OK to freeze	storage condition protect from light, OK to freeze	storage condition OK to freeze, desiccated (hygroscopic), protect from light

Clase de almacenamiento

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Lot/Batch Number

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