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475990 mTOR Inhibitor IV, Ku-63794 - CAS 938440-64-3 - Calbiochem

The mTOR Inhibitor IV, Ku-63794, also referenced under CAS 938440-64-3, controls the biological activity of mTOR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: rel-5-[2-[(2R,6S)-2,6-Dimethyl-4-morpholinyl]-4-(4-morpholinyl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol, Ku-0063794, mTOR Inhibitor IV, Ku-63794

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475990
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Tableau de caractéristiques principal

CAS #Empirical Formula
938440-64-3C₂₅H₃₁N₅O₄

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      Description
      OverviewA cell-permeable pyrido-pyrimidine compound that acts as a highly selective and potent inhibitor against both mTORC1 & mTORC2 (IC50 = ~10 nM against mTOR activity in raptor or rictor immunoprecipitate from HEK293 with 100 µM ATP), with much reduced potency against MKK1 and PI 3-Kα (IC50 ~9 µM) and little or no activity toward more than 200 other protein and lipid kinases, including Akt, ATR, DNA-PK, PDK1, and PI 3-Kβ/γ/δ. Shown to effectively inhibit cellular mTOR phosphorylation on Ser2448/2481 as well as the phosphorylation and activation of mTORC1/2 downstream effector molecules such as Akt, S6K, 4E-BP1, but not RSK or Erk1/2, kinases that are not regulated by mTOR. Although Ku-63794 is shown not to affect IGF-1-induced Akt phosphorylation on Ser308 by PDK1 in mTORC2 knockout MEF cultures, Ku-63794 treatment of mTORC2-expressing MEF cells is shown to inhibit IGF-1-induced Akt Ser308 phosphorylation.
      Catalogue Number475990
      Brand Family Calbiochem®
      Synonymsrel-5-[2-[(2R,6S)-2,6-Dimethyl-4-morpholinyl]-4-(4-morpholinyl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol, Ku-0063794, mTOR Inhibitor IV, Ku-63794
      References
      ReferencesMalagu, K., et al. 2009. Bioorg. Med. Chem. Lett. 19, 5950.
      Garcia-Martinez, J.M., et al. 2009. Biochem. J. 421, 29.
      Product Information
      CAS number938440-64-3
      FormPale yellow solid
      Hill FormulaC₂₅H₃₁N₅O₄
      Chemical formulaC₂₅H₃₁N₅O₄
      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 +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
      Référence GTIN
      475990-5MG 04055977184426

      Documentation

      mTOR Inhibitor IV, Ku-63794 - CAS 938440-64-3 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      mTOR Inhibitor IV, Ku-63794 - CAS 938440-64-3 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      475990

      Références bibliographiques

      Aperçu de la référence bibliographique
      Malagu, K., et al. 2009. Bioorg. Med. Chem. Lett. 19, 5950.
      Garcia-Martinez, J.M., et al. 2009. Biochem. J. 421, 29.
      Fiche technique

      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.

      Revision31-August-2010 RFH
      Synonymsrel-5-[2-[(2R,6S)-2,6-Dimethyl-4-morpholinyl]-4-(4-morpholinyl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol, Ku-0063794, mTOR Inhibitor IV, Ku-63794
      DescriptionA cell-permeable pyrido-pyrimidine compound that acts as a highly selective and potent inhibitor against both mTORC1 & mTORC2 (IC50 = ~10 nM against mTOR activity in raptor or rictor immunoprecipitate from HEK293 with 100 µM ATP), with much reduced potency against MKK1 and PI 3-Kα (IC50 ~9 µM) and little or no activity toward more than 200 other protein and lipid kinases, including Akt, ATR, DNA-PK, PDK1, and PI 3-Kβ/γ/δ. Shown to effectively inhibit cellular mTOR phosphorylation on Ser2448/2481 as well as the phosphorylation and activation of mTORC1/2 downstream effector molecules such as Akt, S6K, 4E-BP1, but not RSK or Erk1/2, kinases that are not regulated by mTOR. Although Ku-63794 is shown not to affect IGF-1-induced Akt phosphorylation on Ser308 by PDK1 in mTORC2 knockout MEF cultures, Ku-63794 treatment of mTORC2-expressing MEF cells is shown to inhibit IGF-1-induced Akt Ser308 phosphorylation.
      FormPale yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number938440-64-3
      Chemical formulaC₂₅H₃₁N₅O₄
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (15 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
      ReferencesMalagu, K., et al. 2009. Bioorg. Med. Chem. Lett. 19, 5950.
      Garcia-Martinez, J.M., et al. 2009. Biochem. J. 421, 29.