528106 | PI 3-Kγ Inhibitor - CAS 648450-29-7 - Calbiochem

528106
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₂H₇N₃O₂S 648450-29-7

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      528106-5MG
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          Plastic ampoule 5 mg
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          Description
          OverviewA cell-permeable thiazolidinedione compound that acts as a potent, selective, and ATP-competitive inhibitor of phosphatidylinositol 3-kinase γ (PI 3-Kγ) (Ki = 7.8 nM; IC50 = 8 nM, 60 nM, 270 nM, 300 nM for p110-γ, α, β and δ-isoforms, respectively). Does not affect the activity of a wide panel of kinases, receptors, enzymes, and ion channels even at concentrations as high as 1 µM. Selectively blocks MCP-1-, but not CSF-1-, dependent Akt phosphorylation and chemotaxis in primary Pik3cg+/+ murine monocytes and in a human monocytic cell line THP-1 (IC50 = 181 nM). Also shown to exhibit in vivo efficacy in reducing neutrophil chemotaxis in murine peritonitis and arthritis models.
          Catalogue Number528106
          Brand Family Calbiochem®
          Synonyms5-Quinoxalin-6-ylmethylene-thiazolidine-2,4-dione, PI 3-K Inhibitor I
          References
          ReferencesBarber, D.F., et al. 2005. Nat. Med. 11, 933.
          Camps, M., et al. 2005. Nat. Med. 11, 936.
          Product Information
          CAS number648450-29-7
          ATP CompetitiveY
          FormPink solid
          Hill FormulaC₁₂H₇N₃O₂S
          Chemical formulaC₁₂H₇N₃O₂S
          ReversibleN
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetPhosphatidylinositol 3-kinase γ (PI 3-Kγ)
          Primary Target IC<sub>50</sub>8 nM, 60 nM, 270 nM, 300 nM for p110-γ, α, β and δ-isoforms, respectively; 181 nM in selectively blocking MCP-1-, but not CSF-1-, dependent Akt phosphorylation and chemotaxis in primary Pik3cg+/+ murine monocytes and in a human mono
          Primary Target K<sub>i</sub>7.8 nM
          Purity≥90% by HPLC
          Physicochemical Information
          Cell permeableY
          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 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
          528106

          References

          Reference overview
          Barber, D.F., et al. 2005. Nat. Med. 11, 933.
          Camps, M., et al. 2005. Nat. Med. 11, 936.
          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.

          Revision14-September-2007 JSW
          Synonyms5-Quinoxalin-6-ylmethylene-thiazolidine-2,4-dione, PI 3-K Inhibitor I
          DescriptionA cell-permeable, potent, selective, and ATP-competitive inhibitor of phosphatidylinositol 3-kinase γ (PI 3-Kγ) (Ki = 7.8 nM; IC50 = 8 nM, 60 nM, 270 nM, 300 nM for p110-γ, α, β and δ-isoforms, respectively). Does not affect the activity of a wide panel of kinases, receptors, enzymes, and ion channels even at concentrations as high as 1 µM. Selectively blocks MCP-1-, but not CSF-1-, dependent Akt phosphorylation and chemotaxis in primary Pik3cg+/+ murine monocytes and in a human monocytic cell line THP-1 (IC50 = 181 nM). Also shown to exhibit in vivo efficacy in reducing neutrophil chemotaxis in murine peritonitis and arthritis models.
          FormPink solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number648450-29-7
          Chemical formulaC₁₂H₇N₃O₂S
          Structure formulaStructure formula
          Purity≥90% by HPLC
          SolubilityDMSO (2.5 mg/ml)
          Storage +2°C to +8°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
          ReferencesBarber, D.F., et al. 2005. Nat. Med. 11, 933.
          Camps, M., et al. 2005. Nat. Med. 11, 936.