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124034 Akt Inhibitor XV, Isozyme-Selective - Calbiochem

124034
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₃₃H₂₉N₇O

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124034-2MG
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      Description
      OverviewA cell-permeable naphthyridinone compound that acts as an allosteric Akt1/2-selective inhibitor (IC50 = 3.5, 42, and 1900 nM against Akt1, Akt2, and Akt3, respectively) in a PH domain-dependent, but not ATP-competitive, manner, with little activity against a panel of more than 160 other kinases, including the related AGC family kinases (inactive at 10 µM against GSK, PDK1, PKA, PKC, and SGK). Effectively inhibits the basal Akt phosphorylation in cancer cells with deregulated Akt pathway activation, including the HCT116 colorectal carcinoma and a panel of breast cancer cell lines (IC50 <500 nM), and suppresses Akt-dependent cell growth both in cultures in vitro (IC50 ≤1 µM) and in mice in vivo (50 to 100 mg/kg, SC). Although also referred to as AKTi-1/2, this is not the same compound as Akt Inhibitor XV (Cat. Nos. 124017 & 124018).
      Catalogue Number124034
      Brand Family Calbiochem®
      Synonyms5-Hydroxy-3-phenyl-2-(4-((4-(5-pyridin-2-yl-1H-1,2,4-triazol-3-yl)piperdin-1-yl)methyl)phenyl)-1,6-naphthyridine
      References
      ReferencesShe, Q.B., et al. 2010. Cancer Cell 18, 39.
      Bilodeau, M.T., et al. 2008. Bioorg. Med. Chem. Lett. 18, 3178.
      She, Q.B, et al. 2008. PLoS One 3, e3065.
      Product Information
      FormWhite powder
      Hill FormulaC₃₃H₂₉N₇O
      Chemical formulaC₃₃H₂₉N₇O
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥97% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage +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 6 months at -20°C.
      Packaging Information
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Akt Inhibitor XV, Isozyme-Selective - Calbiochem MSDS

      Title

      Safety Data Sheet (SDS) 

      Akt Inhibitor XV, Isozyme-Selective - Calbiochem Certificates of Analysis

      TitleLot Number
      124034

      References

      Reference overview
      She, Q.B., et al. 2010. Cancer Cell 18, 39.
      Bilodeau, M.T., et al. 2008. Bioorg. Med. Chem. Lett. 18, 3178.
      She, Q.B, et al. 2008. PLoS One 3, e3065.
      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.

      Revision02-November-2011 RFH
      Synonyms5-Hydroxy-3-phenyl-2-(4-((4-(5-pyridin-2-yl-1H-1,2,4-triazol-3-yl)piperdin-1-yl)methyl)phenyl)-1,6-naphthyridine
      DescriptionA cell-permeable naphthyridinone compound that acts as an allosteric Akt1/2-selective inhibitor (IC50 = 3.5, 42, and 1900 nM against Akt1, Akt2, and Akt3, respectively) in a PH domain-dependent, but not ATP-competitive, manner, with little activity against a panel of more than 160 other kinases, including the related AGC family kinases (inactive at 10 µM against GSK, PDK1, PKA, PKC, and SGK). Effectively inhibits the basal Akt phosphorylation in cancer cells with deregulated Akt pathway activation, including the HCT116 colorectal carcinoma and a panel of breast cancer cell lines (IC50 <500 nM), and suppresses Akt-dependent cell growth both in cultures in vitro (IC50 ≤1 µM) and in mice in vivo (50 to 100 mg/kg, SC). Although also referred to as AKTi-1/2, this is not the same compound as Akt Inhibitor XV (Cat. Nos. 124017 & 124018).
      FormWhite powder
      Chemical formulaC₃₃H₂₉N₇O
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (25 mg/ml)
      Storage +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 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesShe, Q.B., et al. 2010. Cancer Cell 18, 39.
      Bilodeau, M.T., et al. 2008. Bioorg. Med. Chem. Lett. 18, 3178.
      She, Q.B, et al. 2008. PLoS One 3, e3065.