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

475986
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₄H₂₉N₇O₅ 1062169-56-5

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      475986-5MG
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          Plastic ampoule 5 mg
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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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.