124034 Akt Inhibitor XV, Isozyme-Selective - Calbiochem

124034
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₃₃H₂₉N₇O

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      124034-2MG
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          Glass bottle 2 mg
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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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.