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475992 mTOR Inhibitor XII, Torin2 - Calbiochem

Overview

Replacement Information

Products

Catalogue NumberPackaging Qty/Pack
475992-10MG Glass bottle 10 mg
Description
OverviewA 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.
Catalogue Number475992
Brand Family Calbiochem®
Synonyms9-(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
References
ReferencesLiu, Q., et al. 2011. J Med Chem. 54, 1473.
Liu, Q., et al. 2010, J Biol Chem. 284, 8023.
Product Information
FormYellow powder
Hill FormulaC₂₄H₁₅F₃N₄O
Chemical formulaC₂₄H₁₅F₃N₄O
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetMTOR
Primary Target IC<sub>50</sub>2 nM
Purity≥99% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
475992-10MG 04055977184440

Documentation

mTOR Inhibitor XII, Torin2 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

mTOR Inhibitor XII, Torin2 - Calbiochem Certificates of Analysis

TitleLot Number
475992

References

Reference overview
Liu, Q., et al. 2011. J Med Chem. 54, 1473.
Liu, Q., et al. 2010, J Biol Chem. 284, 8023.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision14-June-2013 JSW
Synonyms9-(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
DescriptionA 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.
FormYellow powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₄H₁₅F₃N₄O
Structure formulaStructure formula
Purity≥99% by HPLC
SolubilityDMSO (10 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesLiu, Q., et al. 2011. J Med Chem. 54, 1473.
Liu, Q., et al. 2010, J Biol Chem. 284, 8023.