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475991 | mTOR Inhibitor XI, Torin1 - Calbiochem

475991
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      Overview

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      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      475991-10MG
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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 Image
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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 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.