475991 mTOR Inhibitor XI, Torin1 - Calbiochem

475991
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475991-10MGCN
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      Glass bottle 10 mg
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      Description
      OverviewA cell-permeable pyridinonequinoline derivative that acts as a highly potent, ATP-competitive inhibibitor against mTOR and DNA-PK (IC50 = 4.32 and 6.34 nM, respectively), while inhibiting PI 3-K only at much higher concentrations (IC50 =171 to 533 nM). Effectively inhibits mTORC1-mediated S6K1 phosphorylation in MEF (IC50 = 2 nM) in vitro, as well as mTORC2-mediated Akt and mTORC1-dependent S6 phosphorylations in murine lung and liver in vivo (up to 6 h post single 20 mg/kg i.p. dose). Despite its poor in vivo stability (T1/2 = 4.52 h in mice; 10 mg/kg i.p.), Torin1 is reported to completely suppress U87MG-derived tumor expansion in mice when administered via daily i.p. at a high dosage of 200 mg/kg. Also reported to effectively inhibit cellular mTORC1 functionalities known to be rapamycin-resistant (Cat. Nos. 553210, 553211, and 553212).
      Catalogue Number475991
      Brand Family Calbiochem®
      Synonyms1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one, DNA-PK Inhibitor VI, PI 3-K Inhibitor XVIII
      References
      ReferencesLiu, Q., et al. 2010. J Med Chem. 53, 7146.
      Thoreen, C., et al. 2009. J Biol Chem. 284, 8023.
      Product Information
      CAS number1222998-36-8
      FormYellowish-white powder
      Hill FormulaC₃₅H₂₈F₃N₅O₂
      Chemical formulaC₃₅H₂₈F₃N₅O₂
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationmTOR 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).
      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

      Documentation

      mTOR Inhibitor XI, Torin1 - Calbiochem Certificates of Analysis

      TitleLot Number
      475991

      References

      Reference overview
      Liu, Q., et al. 2010. J Med Chem. 53, 7146.
      Thoreen, C., et al. 2009. 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.

      Revision04-July-2013 JSW
      Synonyms1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one, DNA-PK Inhibitor VI, PI 3-K Inhibitor XVIII
      DescriptionA cell-permeable pyridinonequinoline derivative that acts as a highly potent, ATP-competitive inhibibitor against mTOR and DNA-PK (IC50 = 4.32 and 6.34 nM, respectively, in cell-free kinase assays), inhibiting class I (IC50 =171, 250, and 564 nM, respectively, against P110γ, P110α/P85α, and P110δ/P85α, respectively), class II (IC50 =176 and 564 nM, respectively, against C2α, and C2β, respectively), and class III (IC50 = 533 nM against hVPS34) PI 3-K only at much higher concentrations. Effectively inhibits mTORC1-mediated S6K1 Thr389 phosphorylation in MEF cultures (IC50 = 2 nM) in vitro, as well as mTORC2-mediated Akt Ser473 and mTORC1-dependent S6 Ser235/236 phosphorylations in murine lung and liver in vivo (up to 6 h after single i.p. dose at 20 mg/kg). Despite its poor in vivo stability (T1/2 = 4.52 h in mice; 10 mg/kg i.p.), Torin1 is reported to completely suppress U87MG-derived tumor expansion in mice when administered via daily i.p. at a high dosage of 200 mg/kg. Also reported to effectively inhibit cellular mTORC1 functionalities known to be rapamycin-resistant (Cat. Nos. 553210, 553211, and 553212).
      FormYellowish-white powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1222998-36-8
      Chemical formulaC₃₅H₂₈F₃N₅O₂
      Structure formulaStructure formula
      Purity≥99% by HPLC
      SolubilityDMSO (2 mg/ml)
      Storage +2°C to +8°C
      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.
      Toxicity Standard Handling
      ReferencesLiu, Q., et al. 2010. J Med Chem. 53, 7146.
      Thoreen, C., et al. 2009. J Biol Chem. 284, 8023.