475986 mTOR Kinase Inhibitor II, WYE-354 - CAS 1062169-56-5 - Calbiochem

475986
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Key Spec Table

Empirical FormulaCAS #
C₂₄H₂₉N₇O₅1062169-56-5

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      Description
      OverviewA cell-permeable pyrazolopyrimidine compound that acts as a potent and ATP-competitive mTOR inhibitor (IC50 = 5 nM with S6K as the substrate and 100 µM ATP) with much reduced activity against PI 3-Kα or PI 3-Kγ (IC50 = 1.89 and 7.37 µM, respectively) and little or no activity toward 24 other kinases (IC50 >50 µM). WYE-354 is equally potent against mTORC1 and mTORC2 activities in HEK293 immune complex kinase assays using S6K and Akt as the respective substrate (IC50 <200 nM; [ATP] = 100 µM) and effectively blocks cellular phosphorylation of S6K on T389 and Akt on S473 both in cultures and in a murine xenograft model, resulting in a significant suppression of PC3MM2-derived tumor growth (by 86% on day 7; 50 mg/kg, i.p twice per day) in vivo.
      Catalogue Number475986
      Brand Family Calbiochem®
      SynonymsMethyl-4-(6-{4-[(methoxycarbonyl)amino]phenyl}-4-morpholin-4-yl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate, mTOR Inhibitor II
      References
      ReferencesYu, K., et al. 2009. Cancer Res. 69, 6232.
      Zask, A., et al. 2009. J. Med. Chem. 52, 5013.
      Product Information
      CAS number1062169-56-5
      FormWhite solid
      Hill FormulaC₂₄H₂₉N₇O₅
      Chemical formulaC₂₄H₂₉N₇O₅
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥98% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage -20°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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      mTOR Kinase Inhibitor II, WYE-354 - CAS 1062169-56-5 - Calbiochem Certificates of Analysis

      TitleLot Number
      475986

      References

      Reference overview
      Yu, K., et al. 2009. Cancer Res. 69, 6232.
      Zask, A., et al. 2009. J. Med. Chem. 52, 5013.
      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.

      Revision17-September-2010 RFH
      SynonymsMethyl-4-(6-{4-[(methoxycarbonyl)amino]phenyl}-4-morpholin-4-yl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate, mTOR Inhibitor II
      DescriptionA cell-permeable pyrazolopyrimidine compound that acts as a potent and ATP-competitive mTOR inhibitor (IC50 = 5 nM with S6K as the substrate and 100 µM ATP) with much reduced activity against PI 3-Kα or PI 3-Kγ (IC50 = 1.89 and 7.37 µM, respectively) and little or no activity toward 24 other kinases (IC50 >50 µM). WYE-354 is equally potent against mTORC1 and mTORC2 activities in HEK293 immune complex kinase assays using S6K and Akt as the respective substrate (IC50 <200 nM; [ATP] = 100 µM) and effectively blocks cellular phosphorylation of S6K on T389 and Akt on S473 both in cultures and in a murine xenograft model, resulting in a significant suppression of PC3MM2-derived tumor growth (by 86% on day 7; 50 mg/kg, i.p twice per day) in vivo.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1062169-56-5
      Chemical formulaC₂₄H₂₉N₇O₅
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage -20°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 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesYu, K., et al. 2009. Cancer Res. 69, 6232.
      Zask, A., et al. 2009. J. Med. Chem. 52, 5013.