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475992 mTOR Inhibitor XII, Torin2 - Calbiochem

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475992
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概要

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475992-10MGCN
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      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
      カタログ番号 GTIN
      475992-10MGCN 04055977184440

      Documentation

      mTOR Inhibitor XII, Torin2 - Calbiochem (M)SDS

      タイトル

      英語版製品安全データシート((M)SDS) 

      mTOR Inhibitor XII, Torin2 - Calbiochem 試験成績書(CoA)

      タイトルロット番号
      475992

      参考資料

      参考資料の概要
      Liu, Q., et al. 2011. J Med Chem. 54, 1473.
      Liu, Q., et al. 2010, J Biol Chem. 284, 8023.
      データシート

      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.